Vasantidevi Patil Institute of Pharmacy
UniversityKodoli, Maharashtra, India
Research output, citation impact, and the most-cited recent papers from Vasantidevi Patil Institute of Pharmacy (India). Aggregated across the NobleBlocks index of 300M+ scholarly works.
Top-cited papers from Vasantidevi Patil Institute of Pharmacy
The global incidence of bloodstream infections (BSIs) is rising, necessitating the development of effective therapeutic strategies to achieve complete eradication. This study focuses on the synthesis of silver nanoparticles (AgNPs) functionalized with Clematis gouriana extract (CG) (CG-AgNPs) as a potential alternative to conventional treatments for combating BSIs caused by bacterial pathogens. AgNPs were synthesized by reducing silver nitrate (AgNO₃) using CG extract. The formation of CG-AgNPs was confirmed through UV-Vis spectroscopy, while their characterization included the determination of mean particle size and zeta potential. Elemental composition was analyzed using energy-dispersive X-ray (EDX) spectroscopy. The in vitro antibacterial efficacy of CG-AgNPs was assessed through multiple assays, including a time-kill assay, a film bioadhesion assay, and measurement of reactive oxygen species (ROS) generation. SPR (surface plasmon resonance) has been employed to validate the development of AgNPs by observing a colour shift to dark brown. The mean particle size and zeta potential of the CG-AgNPs were found to be 38 ± 2 nm (PDI 0.104 ± 0.03) and -31.2 ± 1.4 mV, respectively. Additionally, E-XRD results show that the prepared AgNPs comply with the silver presence. The minimum inhibitory concentrations (MIC) and minimum bactericidal concentrations (MBC) of the CG-AgNPs against Staphylococcus aureus ( S. aureus ) were observed to be 6.25 ± 0.8 µg/mL and 13.5 ± 2.4 µg/mL, respectively.Similarly, the MIC and MBC of CG-AgNPs against Escherichia coli ( E. coli ) were found to be 13.5 ± 1.5 μg/mL and 26 ± 2.8 μg/mL, respectively. CG-AgNPs also prevented biofilm formation and bacterial adhesion in a dose-dependent manner; 100% inhibition was achieved in 48 h at MBC. In addition, CG-AgNPs remarkably escalated the ROS level within cells, indicating their mechanism of antimicarobial activity. The findings of this study demonstrate that CG-AgNPs synthesized via green synthesis exhibit significant antibacterial activity, highlighting their potential as an effective alternative for the treatment of BSIs. However, further in vivo studies are required to optimize a suitable dosage form and validate their therapeutic efficacy against bacterial infections in clinical settings. • The quest of identify novel approach to address the escalating global burden of blood stream infections (BSIs) by synthesizing silver nanoparticles by green synthesis. • A The synthesis process involved reducing silver nitrate (AgNO 3 ) solution with CG extract, yielding AgNPs characterized by UV-visible spectroscopy particles size and antibacterial activity etc. • The CG-AgNPs induced apoptosis and elevated intracellular reactive oxygen species (ROS) levels in treated cells. • CG-AgNPs demonstrated notable antibacterial activity against both S. aureus and E. coli , with MIC and MBC values indicating effective inhibition. • These findings suggest CG-AgNPs synthesized through green synthesis offer significant advancements antibacterial interventions. Further research is warranted to validate their efficacy in vivo for treatment of BSIs
Nanoparticles can offer important advantages over the administration of conventional drugs in terms of high stability, high specificity, high drug transport capacity, controlled release capacity, possibility of use in different routes of administration and the ability to administer drugs both hydrophilic and hydrophobic molecules. Nanoparticles are being used for various purposes, from medical treatments, use in various branches of the production industry such as solar and for energy storage, to a wide incorporation obsessed with various everyday materials such as cosmetics or dress, optical devices, catalytic, bactericidal, electronics, sensor technology, biological labelling and treatment of some cancers. Nanoparticles can be chemically or biologically synthesized. This review focuses on the need to develop nanoparticles, advantages, disadvantages, synthesis, properties, applications of nanoparticles exist in different forms. Nanoparticles are very capable in selective tumour contact cancer therapy due to their small size and modifiability. These particles consist of pure active pharmaceutical ingredients and are stabilized regularly with surfactant. Nanoparticles are tiny materials that have particle sizes in the range of 1 to 1000 nm.
Objective The present study aimed to identify a safe and effective non-oncology drug cocktail as an alternative to toxic chemotherapeutics for hepatocellular carcinoma (HCC) treatment. The assessment of cytotoxicity of cocktail (as co-adjuvant) in combination with chemotherapeutic docetaxel (DTX) is also aimed. Further, we aimed to develop an oral solid self-emulsifying drug delivery system (S-SEDDS) for the simultaneous delivery of identified drugs.Significance The identified non-oncology drug cocktail could overcome the shortage of anticancer therapeutics and help to reduce cancer-related mortality. Moreover, the developed S-SEDDS could be an ideal system for concurrent oral delivery of non-oncology drug combinations.Methods The non-oncology drugs (alone and in combinations) were screened in vitro for anticancer effect (against HepG2 cells) using (3-(4,5-dimethylthiazolyl-2)-2,5-diphenyltetrazolium bromide; MTT) dye assay, and cell cycle arresting and apoptotic behaviors using the fluorescence-activated cell sorting (FACS) technique. The S-SEDDS is composed of drugs such as ketoconazole (KCZ), disulfiram (DSR), tadalafil (TLF), and excipients like span-80, tween-80, soybean oil, Leciva S-95, Poloxamer F108 (PF-108), and Neusilin® US2 (adsorbent carrier), which was developed and characterized.Results The cocktail composed of KCZ, DSR, and TLF has showed substantial cytotoxicity (at the lowest concentration of 3.3 pmol), HepG2 cell arrest at G0/G1 and S phases, and substantial cell death via apoptosis. The DTX inclusion into this cocktail has further resulted in increased cytotoxicity, cell arrest at the G2/M phase, and cell necrosis. The optimized blank liquid SEDDS that remains transparent without phase separation for more than 6 months is used for the preparation of drug-loaded liquid SEDDS (DL-SEDDS). The optimized DL-SEDDS with low viscosity, good dispersibility, considerable drug retention upon dilution, and smaller particle size is further converted into drug-loaded solid SEDDS (DS-SEDDS). The final DS-SEDDS demonstrated acceptable flowability and compression characteristics, significant drug retention (more than 93%), particle size in nano range (less than 500 nm), and nearly spherical morphology following dilutions. The DS-SEDDS showed substantially increased cytotoxicity and Caco-2 cell permeability than plain drugs. Furthermore, DS-SEDDS containing only non-oncology drugs caused lower in vivo toxicity (only 6% body weight loss) than DS-SEDDS containing non-oncology drugs with DTX (about 10% weight loss).Conclusion The current study revealed a non-oncology drug combination effective against HCC. Further, it is concluded that the developed S-SEDDS containing non-oncology drug combination alone and in combination with DTX could be a promising alternative to toxic chemotherapeutics for the effective oral treatment of hepatic cancer.
OBJECTIVE: The peculiar aim of this study is to discover and identify the most effective and potential inhibitors against the most influential target ERα receptor by in silico studies of 45 phytochemicals from six diverse ayurvedic medicinal plants. METHODS: The molecular docking investigation was carried out by the genetic algorithm program of AutoDock Vina. The molecular dynamic (MD) simulation investigations were conducted using the Desmond tool of Schrödinger molecular modelling. This study identified the top ten highest binding energy phytochemicals that were taken for drug-likeness test and ADMET profile prediction with the help of the web-based server QikpropADME. RESULTS: Molecular docking study revealed that ellagic acid (-9.3 kcal/mol), emodin (-9.1 kcal/mol), rhein (-9.1 kcal/mol), andquercetin (-9.0 kcal/mol) phytochemicals showed similar binding affinity as standard tamoxifen towards the target protein ERα. MD studies showed that all four compounds possess comparatively stable ligand-protein complexes with ERα target compared to the tamoxifen-ERα complex. Among the four compounds, phytochemical rhein formed a more stable complex than standard tamoxifen. ADMET studies for the top ten highest binding energy phytochemicals showed a better safety profile. CONCLUSION: Additionally, these compounds are being reported for the first time in this study as possible inhibitors of ERα for treating breast cancer, according to the notion of drug repurposing. Hence, these phytochemicals can be further studied and used as a parent core molecule to develop innovative lead molecules for breast cancer therapy.
This research aims to formulate and characterize transfersomes containing curcumin (CUR-TFS) for the enhanced melanoma activity. Thin film hydration was used to prepare the CUR-TFS with Phospholipon® 90 G and sodium cholate. The formulated transfersomes were studied for their size, zeta potential (ZP), entrapment efficiency (EE), skin penetration and ex-vivo skin permeation. Differential scanning calorimetry (DSC) and x-ray diffraction (XRD) were used to determine the physical state of the drug in the optimized curcumin transfersomes (OPT-CUR-TFS). In vitro cytotoxicity, cellular uptake, live and dead cell assay, soft agar colony assay, and apoptosis analysis were carried out using the A375 melanoma cell line. The size and EE of the OPT-CUR-TFS were 191 ± 5.25 nm and 91.72 ± 0.36%, respectively. When compared to conventional liposomes, transfersomes showed significantly increased drug permeation and deposition in the skin layers. The penetration of transfersomes into the deeper skin layers was illustrated through fluorescence microscopy. The DSC and XRD analysis suggested that CUR in transfersomes was amorphous, demonstrating its successful encapsulation inside the transfersomes. The OPT-CUR-TFS was found to significantly decrease the cell viability in A375 cell lines due to their higher cellular uptake. In addition, the OPT-CUR-TFS showed enhanced antiproliferative action by suppressing the clonogenic potential of A375 cells. Furthermore, the OPT-CUR-TFS induced apoptosis-mediated cell death in A375 cells. These findings could offer a powerful justification for CUR transfersomes as a viable treatment strategy for the management of melanoma.
Polymeric micelles have been extensively studied as nanocarriers for hydrophobic drugs. They can be designed to have the intensity of duration and blood circulation, as well as binding specificity to certain highly stressed receptors on the surface of cancer cells. y. The incorporation of these agents into nanoparticles reduces the adverse effects of standard chemotherapy on healthy tissues. Such nanoparticles, considered to be drug-transporting vehicles, are versatile and include micelles, liposomes, dendrimers, nanocapsules, nanospheres and more. Polymeric micelles have been extensively studied as nanocarriers for hydrophobic drugs. They can be designed to have the intensity of duration and circulation, as well as binding specifications to certain more receptors expressed on the surface of cancer cells. When these drug-induced nanoparticles reach the plant surface, an external stimulus, such as ultrasound, can be used to introduce local and temporary drug release.
Emulsion stability is vital for effectiveness, ensuring uniform distribution of droplets and preventing phase separation. Instability can lead to inconsistent performance and reduced therapeutic benefits. Thus, our research endeavors were directed toward the design and characterization of a sericin (SN) stabilized quercetin (QRN) emulgel (EG), specifically tailored for diabetic wound healing. Employing a two-factor, 3-level factorial design SN-stabilized QRN emulgel (QSEG) was prepared and the influence of varying percentages of olive oil and SN on zeta potential, globule size, and entrapment efficiency (%) was scrutinized. The optimized QRN emulgel (QSEG), composed of 10% oil and 5% SN (QSE-6), showcased a diminutive globule size of 809.2 ± 21.3 nm alongside an elevated zeta potential of −42.9 ± 3.79 mV. Submicron-sized spherical globules were observed without any signs of coalescence, confirmed by surface morphology analysis. FTIR showed compatibility, while DSC and XRD confirmed that QRN was amorphized and evenly dispersed within the emulgel. In-vitro scratch assays manifested reduced intercellular distances and wound closure, indicative of potent wound healing attributes of QSEG. QSEG demonstrated notable antibacterial efficacy against Escherichia coli (E. coli), with minimum inhibitory concentrations (MIC) and minimum bactericidal concentrations (MBC) of 3.125 ± 0.4 and 6.25 ± 1.2 μg/mL, respectively, surpassing that against Staphylococcus aureus (S.aureus). Cytotoxicity assays evidenced diminished toxicity toward fibroblast cells. Furthermore, in-vivo wound healing studies unveiled significant (p ˂ 0.001) enhancements with QSEG compared to QRN-treated and control groups. Our findings underscore SN’s role as a natural stabilizer, synergistically enhancing QSEG’s diabetic wound healing potential. Conclusively, QSEG emerges as a promising alternative to conventional diabetic wound healing treatments, offering inherent medicinal benefits.
The quest to improve the effectiveness of anti-breast cancer medicines has diverted the researchers to explore a topical administration of drugs onto the breast. The different parts of Acacia senegal plant (ASP) have showed promising anticancer effects but with marred efficacy. Present research was aimed to develop, optimize, and characterize ASP root and stem bark extract (ASPE)-loaded ethosomes (ASPE-ETH) as carriers for improved topical treatment of breast cancer. Ethosomes were formulated and optimized using 3 2 factorial design. Optimized ASPE-ETH was evaluated for vesicle size, zeta potential, in vitro skin permeation, cytotoxicity, cellular uptake and live deal cell assay etc . ASPE-ETH appeared as unilamellar nano-vesicles (219 ± 7 nm) with nearly round in shape and had zeta potential of 32.1 ± 2.43 mV. ASPE-ETH demonstrated significant (p < 0.01) in vitro cytotoxicity (IC 50 : 47.68 ± 1.83 µg/mL) than ASPE (184.3 ± 3.68 µg/mL) against MCF-7 Cells. Compared to ASPE, ASPE-ETH treatment caused apoptosis of large proportion of cancer cells. The above results could be correlated to the increased cell uptake of ASPE-ETH as shown by in vitro cell uptake study. Furthermore, the in-vitro skin permeation study results revealed enhanced penetration of ASPE-ETH into the deeper layers of the skin. The study results revealed that ASPE-ETH could be used as a potential alternative treatment approach to conventional chemotherapy. However; further in vivo animal studies are required to establish its efficacy in the treatment of breast cancer. • Acacia senegal ethosomes optimized via 3 2 full factorial design. • Ethosomes: 219 ± 7 nm size, 32.1 ± 2.43 mV zeta potential, optimized for efficacy. • Optimized ethosomes exhibit enhanced cytotoxicity compared to plain extract. • Improved uptake and apoptosis in breast cancer cells with optimized ethosomes. • Ethosomes show deeper skin penetration for targeted breast cancer treatment.
Stem cells are defined as strong clonogenic and regenerative cells and differentiate into multiple cell lines. Stem cells are found in all of us, from the earliest stages of human growth to the end of life. According to the classification of stem cells are divided into 5 types: totipotent, pluripotent, multipotent, oligopotent and unipotent. They are essential for growth, development, maintenance and repair of the brain, bones, muscles, nerves, blood, skin, and other organs. Stem cell therapy continues as a new flexible approach to the treatment of diseases and injuries, with extensive medical benefits. Stock research raises many ethical and scientific questions as well as future challenges. Stem cell therapy, a precursor to a period of cell-based treatment that will one day restore function to those whose lives are now facing the daily challenge, is on its way to recovery. Stem cells have great potential for tissue regeneration and tissue repair but much remains to be learned about their biology, deception and safety before their full therapeutic potential can be discovered. In today’s world, disease control is very exciting and new methods are available to provide quality patient care, on the basis of scientific experiments and practical studies conducted by various institutions and organizations. Mesenchymal stem cells (MSCs) are purchased from most body tissues usually by the placenta and umbilical cord but other sources such as bone marrow found in MSCs are also important as each source will give the cells their own characteristics. They can be used for a variety of heart-related problems, bacterial infections, cirrhosis, liver failure, diabetes, and cancer treatment. A variety of procedures, whether physical or surgical, are available including cell therapy, tissue, osteo-engineering engineering and immunosuppressive tests to treat disease and ensure complete recovery.
Objectives: Bionanocomposites (BNCs) are biopolymers or a natural polymers embedded in a combination of two or more different chemicals using natural carriers or bio. BNCs are widely used in drug formulation and in the development of new drugs for various therapeutic drugs, new dosage forms and in pharmacological medicine. Materials and Methods: Useful and improved melting was achieved by converting selected Biopharmaceutics Classification System (BCS) class II drug into BNCs using natural carriers such as the gums of Moringa oleifera Lam. and Aegle marmelos (L.) Correa, respectively. The current work focuses on the enhancement of the novel natural polymers such as M. oleifera and A. marmelos, used to prepare BNC for BCS class II orlistat using a microwave system designed for the distribution method. The natural polymer helps improve the melting of the dispersion when it converts them into BNC. Definitions of orlistat, natural carriers, and prepared BNCs were developed and studied comparatively. The fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC) study revealed that there was no communication between drug associations and environmental carriers. Results: Crowd reduction studies were conducted to investigate the material that enhances the melting of BNC compounds dissolving and in vitro disposal of BNCs prepared by DSC, scanning electron microscopy, X-ray diffraction studies, and FTIR. BNCs affect orlistat: M. oleifera (OSMO-BNC-1: 3), orlistat: A. marmelos (OSAM-BNC-1: 4) is well developed. Conclusion: Ornat BNCs developed with M. oleifera and A. marmelos provide significant improvements in dissolve and highlight their use in reducing fortification. Additionally, land melting limits were applied and determined for the melting of BNCs prepared using the Hansen Solubility parameters in particular, Hoy's, Fedor and Van Krevelen system and it was found that this report there was a significant increase in the melting of batches prepared for BNCs.
Folliculitis is a common dermatological disorder characterized by inflammation and bacterial infection of hair follicles, most frequently caused by Staphylococcus aureus . The present study aimed to develop a polyherbal silver nanoparticle (PH-AgNPs)–loaded shampoo using a green synthesis approach to exploit phytochemical synergy for enhanced antibacterial efficacy in the management of scalp folliculitis. Silver nanoparticles were synthesized by reducing silver nitrate (AgNO₃) with an aqueous polyherbal extract containing Acacia concinna , Camellia oleifera , Emblica officinalis , and Sapindus mukorossi , which simultaneously acted as reducing and stabilizing agents. The synthesized PH-AgNPs were characterized using UV–visible spectroscopy, dynamic light scattering (DLS), zeta potential analysis, and energy-dispersive X-ray spectroscopy (EDX). The nanoparticles exhibited a mean particle size of 87 ± 2 nm, a polydispersity index of 0.218 ± 0.07, and a zeta potential of −33.2 ± 2.1 mV, indicating good colloidal stability. Antibacterial evaluation demonstrated potent activity against S. aureus , with a minimum inhibitory concentration (MIC) of 0.8 ± 0.06 µg/mL and a minimum bactericidal concentration (MBC) of 3.12 ± 0.5 µg/mL. Furthermore, PH-AgNPs significantly inhibited bacterial adhesion and biofilm formation in a dose-dependent manner, achieving complete biofilm inhibition at MBC within 48 h. Incorporation of PH-AgNPs into a shampoo base provides a green, polyherbal-synergistic topical nanotherapeutic system with promising potential for the treatment of bacterial folliculitis, warranting further in vivo and clinical investigations to confirm therapeutic safety and efficacy. • Polyherbal silver nanoparticles (PH-AgNPs) were synthesized using a green approach from Acacia concinna , Camellia oleifera , Emblica officinalis , and Sapindus mukorossi . • The synthesized PH-AgNPs showed nanoscale size (87 ± 2 nm) and high stability (zeta potential −33.2 ± 2.1 mV). • PH-AgNPs exhibited strong antibacterial activity against Staphylococcus aureus with MIC = 0.8 μg/mL and MBC = 3.12 μg/mL. • The PH-AgNPs effectively inhibited bacterial adhesion and biofilm formation, demonstrating potential for treating scalp folliculitis.
Background: Breast cancer is the leading and most frequent cancer among women worldwide, with rapidly growing new cases diagnosed, surpassing lung cancer. The current study aims to design, optimize and characterize Letrozole (LTZ) Loaded Ethosomes (LTZ-ETH) for the treatment of breast cancer. Materials and Methods: Ethosomes were optimized using a two-factor, three-level (32) factorial design technique. The ethosomes were characterized by vesicle size, zeta potential and entrapment efficiency. The optimized LTZ-ETH was tested for surface morphology and in vitro cytotoxicity. Results: The optimized LTZ-ETH has flawed round-shaped unilamellar structures with an average vesicle size of 218.6 ± 5 nm and an entrapment efficiency of 92.45±3.42%. Optimized LTZ-ETH demonstrated significant (p<0.01) in vitro cytotoxicity (IC50: 23.27±1.48 μg/mL) than LTZ (58.70±2.46 μg/mL) against MCF-7 Cells. Compared to LTZ, LTZ-ETH treatment caused apoptosis of large proportion of cancer cells. The above results could be correlated to the increased cell uptake of LTZ-ETH as shown by in vitro cell uptake study. Furthermore, the in vitro skin permeation study results revealed enhanced penetration of LTZ-ETH into the deeper layers of the skin. Conclusion: The study results revealed that LTZ-ETH could be used as a potential alternative treatment approach to conventional chemotherapy. However; further in vivo animal studies are required to establish its efficacy in the treatment of breast cancer.
Breast Cancer Gene 1 (BRCA1) offers a potential approach for ERα repression by blocking cyclin D1’s interaction with ERα, which prevents cells from growing and dividing too rapidly or uncontrollably. When BRCA1 levels are low, BRCA1 mimetics fit into the BRCA1-binding pocket within ERα, mimicking the ability of BRCA1 to inhibit ERα activity. This study aims to identify a novel class of lead molecules for BRCA1 mimetics for ER-positive breast cancer, distinct from conventional antiestrogen therapies in their mechanism of action. In this article, coumarin thiosemicarbazone hybrids were synthesized from 7-hydroxy 4-methyl coumarin/4-hydroxy coumarin and thiosemicarbazide with different aldehydes and evaluated for their ERα repression activity. The most active compounds in the series, 9b, 9l, and 9m, exhibited significant potency with an IC50 value of 14.49 µM, 35.08 µM and 42.12 µM, respectively, compared to raloxifene (reported) as the positive control with an IC50 value of 13.7 µM. The gene expression study confirmed the downregulation of the cyclin D1 gene for the compounds 9l (−0.217) and 9m (−0.214). Similarly, the downregulation of the BCL2 gene for the compounds 9b (−0.373), 9l (−0.320), and 9m (−0.376). Also, molecular docking studies and MMGBSA were performed to determine key interactions between compounds and ERα at the BRCA1 binding pocket (AA 338–387). In silico, ADMET properties were executed to illustrate the druggability and safety of the novel derivatives. In silico, in vitro, and gene expression studies revealed that among all the compounds, 9b, 9l, and 9m are promising candidates for the development of lead molecules targeting ERα inhibitors for breast cancer treatment. Moreover, the concept of ERα repression with small molecules as BRCA1 mimetics is novel. In general, it can be concluded that these compounds can serve as promising leads to the design of potential BRCA1 mimetics.
In the pursuit of effective diabetes management, inhibiting α-amylase activity stands as a critical strategy. This inhibition regulates post-meal blood sugar levels by retarding carbohydrate digestion, mitigating abrupt glucose spikes, and enhancing glycemic control, thus safeguarding against diabetic complications. In this study, molecular docking and DFT investigations were conducted on phytochemical compounds sourced from various plants, unveiling Conanine, Friedelin, Sennoside A, and Sennoside B as promising candidates. These compounds demonstrated robust binding affinities exceeding -9 kcal/mol when targeted against α-amylase, with Conanine leading the charge at -9.5 kcal/mol. Sennoside A and Sennoside B exhibited their effectiveness by forming multiple hydrogen bonds with the enzyme, underlining their strong binding interactions. Furthermore, DFT calculations affirmed the favorable chemical reactivity profiles of these ligands, characterized by significant HOMO-LUMO energy gaps. This research offers valuable insights into potential therapeutic agents for diabetes management, promising better glycemic control and a brighter future for individuals with diabetes.
Background: Increasing antifungal resistance, poor mucosal retention, and systemic side effects limit the effectiveness of currently available drugs. This study explores a novel topical nanotherapeutic approach for the targeted treatment of vulvovaginal candidiasis (VVC), employing green-synthesized silver nanoparticles (AgNPs) derived from Ascophyllum nodosum (AN) and incorporating ibrexafungerp citrate (IBC) into a liposomal formulation. Methods: AgNPs were biosynthesized using AN extract and characterized. Liposomes were prepared by thin-film hydration, and optimised using Central Composite design and characterized and optimized. Optimised liposomes, co-loaded with IBC and AN-AgNPs, were incorporated into a Carbopol-CMC-based topical gel. Results: FTIR shifts in the –OH (3332.31 cm−1) and carbonyl (1636.87 cm−1) bands with reduced intensity confirmed their involvement in Ag+ reduction and nanoparticle surface coordination, while the persistence of the 1015 cm−1 band indicated the role of polysaccharides in capping and stabilizing the AN-AgNP. Characterization of the optimized liposomes (IBCL-11) revealed a particle size of 127.2 nm, a zeta potential of −43.8 mV, and a polydispersity index (PDI) of 0.35. Transmission Electron Microscopy (TEM) confirmed the presence of intact, spherical vesicles, while Differential Scanning Calorimetry (DSC) and X-ray diffraction (XRD) validated the molecular dispersion and amorphous characteristics of the films. In vitro evaluations of the IBC liposomal gel demonstrated a sustained drug release of 72.6% over 24 h, alongside enhanced drug penetration across all skin layers. Antifungal assays highlighted the formulation’s potent efficacy, yielding Minimum Inhibitory Concentration (MIC) and Minimum Fungicidal Concentration (MFC) values below 1 µg/mL. Furthermore, the treatments exhibited strong anti-biofilm properties; at MIC and MBC levels, AN-AgNPs achieved biofilm reductions of 45.27 ± 3.16% and 27.62 ± 2.13%, respectively, whereas IBCL-11 produced reductions of 34.25 ± 2.43% and 16.28 ± 1.72%. Conclusion: Ultimately, this study successfully developed an eco-friendly liposomal formulation co-loaded with AN-AgNPs and IBC, offering a promising and targeted therapeutic approach for the treatment of vulvovaginal candidiasis.
Background: Cancer is a life-threatening disease which is a major threat to global health which continues to affect predominantly in developing nations. Present research work has been oriented towards the determination of the anticancer potential of camptothecin (CPT) as herbal medicine for the treatment of prostate and lung carcinoma. Methods: Structural determination of camptothecin has been performed by different analytical techniques where anticancer potential was tested by MTT assay, Flow cytometry and DAPI on A549 and LNCaP cells lines. Results: FTIR spectra of camptothecin showed peaks related to specific structure which is nearly equal to standard structure of CPT. NMR spectra of camptothecin showed specific peaks in the region of delta 8.686 - 5.279, the signals of H-7 related to structural features similar to camptothecin. LCMS spectra of camptothecin showed mean retention time at 3.620 and covered 100 % area along with mass spectra gives precursor m/z peak at 349.2 [M+H]+ matches to standard molecular weight of camptothecin. CPT has been used as competent alternative to systemic chemotherapy to cure lung and prostate carcinoma having IC50 value 3.421 μg /ml and 5.253μg /ml respectively. CPT successfully induces apoptosis in A549 and LNCaP cell lines 72.12 ± 3.45 % and 66.41 ± 4.50 % as compared to control 4.28 ± 1.78 and 1.52 ± 0.58 respectively which was proved by DAPI and flow cytometry. Conclusions: Chemical fingerprinting and structural elucidation confirmed that isolated moiety was camptothecin and it has great potential in treatment of lung and prostate carcinoma as a competent alternative to chemotherapy in the form of herbal medicine.
The first-line chemotherapy is associated with chief shortfalls such as non-specific distribution causing severe dose-dependent toxicities and development of tumor resistance.The current preliminary study aimed to identify the safe and effective non-oncology drugs as an alternative to toxic chemotherapeutics to treat osteosarcoma, and overcome new drug's shortage and development challenges.The different category non-oncology drugs (alone and in combinations) were screened for in vitro cytotoxicity behavior via MTT dye reduction assay and cell cycle arresting behavior using flow cytometer against human osteosarcoma (Saos-2 and MG-63) cells.The molecular docking of selected therapeutics was executed against cyclin-dependent kinase 1 (CDK1), cell cycle regulator overexpressed in cancer.The identified combination was further tested for in vivo toxicities in rats at two different doses.The current study revealed niclosamide (NSD), ketoconazole (KCZ), simvastatin (SVN) combination that causes substantial cytotoxicity (IC50 values are in picomoles) at 1:1:3 molar ratio when compared to other molar ratios.This combination has also caused substantial arrest of Saos-2 and MG-63 cells at S and G2/M phase.Additionally, all three drugs demonstrated better interaction with CDK1 indicating anticancer potential via inhibition of CDK1.Furthermore, the in vivo toxicity study revealed no significant changes in hematological and biochemical parameters, body weights of rats, weights of vital organs, daily food and water intake, and general behavior of rats.The obtained preliminary results revealed the potential application of this combination on non-oncology drugs in the safe and effective treatment of osteosarcoma.However, further in-depth studies are required before clinical application.
Cancer is the leading cause of death, and incidences are increasing significantly and patients suffering from it desperately need a complete cure from it. The science of using an already-invented drug that has been approved by the FDA for a new application is known as “drug repurposing.” Currently, scientists are drawn to drug repositioning science in order to investigate existing drugs for newer therapeutic uses and cancer treatment. Because of their unique ability to target cancer cells, recently repurposed drugs and the liposomal approach are effective in the treatment of cancer. Liposomes are nanovesicles that are drastically flexible, rapidly penetrate deeper layers of cells, and enhance intracellular uptake. More importantly, liposomes are biocompatible, biodegradable; entrap both hydrophobic and hydrophilic drugs. This chapter summarizes various approaches to drug repurposing, as well as drug repurposing methods, advantages and limitations of drug repurposing, and a liposomal approach to using repurposed drugs in cancer targeting. This chapter also summarizes liposomal structure, drug loading, and the mechanism of liposomes in targeted cancer treatment. The lipid-based liposomal approach is emerging as a powerful technique for improving drug solubility, bioavailability, reducing side effects, and improving the therapeutic efficacy of repurposed drugs for cancer treatment.
Background: Acne vulgaris is a disorder related to the skin (pilosebaceous), which is mainly caused by the formation of seborrhea, comedones, etc. It mainly affects the face, back, head and oil glands. In spite of the potent antimicrobial, anti-inflammatory and antibacterial potential of Dapsone (DPS), it has hurdles like poor water solubility and bioavailability. The objective of current research is to design, optimize and characterize Dapsone Emulgel (DPSE) for the treatment of acne vulgaris. Materials and Methods: DPSE was prepared by an oil-in-water emulsion-based method and optimized using a central composite design and the effects of carbapol-934 and liquid paraffin concentrations on drug release, viscosity and spread ability were assessed. The optimized DPSE formulation was evaluated for pH, viscosity, extrudability, spread ability, globule size, zeta potential, drug content, in vitro antibacterial assay, time-kill and film bio-adhesion assay. Results: Results revealed that the optimized DPSE exhibited a mean globule size of 382.3±4.17 nm with a PDI of 0.230.010 and a zeta potential of -21.8±3.21 mV with a drug content of 96.95±1.71% of dapsone. Optimized DPSE showed good viscosity (39481±2.645 cps), spread ability (14.68±0.02 g/cm/sec) and excellent extrudability. Optimized DPSE displayed MICs (Minimum Inhibitory Concentrations) and MBCs (Minimum Bactericidal Concentrations) of 10±1.5 μg/mL and 21±2 μg/mL, respectively, against P. acne when compared to S. aureus. (MIC-54±2.5 μg/mL MBC-98±4 μg/mL). Furthermore, DPSE inhibited biofilm formation and bacterial adhesion in a dose-dependent manner, with 100% inhibition obtained in 48 hr at MBC. The percentage of live bacteria in the biofilm treated with MBC and the MIC concentration of DPSE was 31.54±1.32% and 62.91±3.12%, respectively, in comparison to the control
HPLC method development and validation play important role in the discovery, development and manufacture of pharmaceutical products. This article mainly focuses on the optimization of HPLC conditions and other important perspectives during method development and validation. Various critical steps related to analytical method development and validation is discussed. A sequence of events required for method development and analytical validation are described. The steps involved in developing a stability-indicating HPLC method influences the analysis of degradation products/impurities in stability study and its validation demonstrate the suitability for its intended purpose.