Journal of Applied Pharmaceutical Research (JOAPR)
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Review on advancements in liposomal dosage forms with newer methodologies and clinical perspectives
Get PDFBackground: Liposomes are widely used as drug delivery systems because of their reduced systemic toxicity. Over the past few decades, numerous drug-loaded liposomes have been approved for clinical use in the treatment of cancer, viral, and fungal infections. Various liposomal formulations have progressed to later phases of clinical trials. Liposomes are spherical vesicles composed of a single or multiple phospholipid bilayers surrounding an aqueous core. Drug-loaded liposomes can exhibit controlled or targeted drug delivery, low immunogenicity, high biocompatibility, biodegradability, prolonged drug half-life, increased efficiency, reduced systemic toxicity, and enhanced pharmacokinetic properties. Methodology: This review article addresses the characteristics and types of liposomes; novel methods for their preparation, such as the Supercritical Anti-solvent Method and the Dual Asymmetric Centrifugation Method; lipid preferences; future directions for liposomes; marketed liposomal formulations; and associated patents. Results and Discussion: It has the potential to protect the drug against degradation. The aforementioned drug delivery system increases in vivo drug distribution toward target sites. PEGylated liposomes can prolong circulation time. It requires expertise in techniques, such as thin-film hydration and reverse-phase evaporation, for preparation. It has been utilized in nanomedicine. This particular delivery system requires characterizations like size, drug loading, drug release, etc. Conclusion: Liposome-embedded delivery systems advance nanotechnology and biopharmaceutics. The role of modern medicine has continued to expand, particularly in the management of chronic diseases
Development and characterization of nanocrystals for solubility enhancement of poorly soluble drug azelnidipine
No full textBackground: Azelnidipine is a BCS Class II drug characterized by low solubility and high permeability, resulting in approximately 50% bioavailability. The limited bioavailability of this compound is primarily attributed to its poor aqueous solubility. Therefore, enhancing the solubility and dissolution rate of Azelnidipine is essential to improve its bioavailability. This study aimed to develop and characterize Azelnidipine Nanocrystals to enhance the solubility and dissolution rate of Azelnidipine, which is currently in micronized form. Methodology: Azelnidipine nanocrystals were prepared via antisolvent precipitation. Azelnidipine nanocrystals were synthesized using PVP and SLS as stabilizers via a precipitation process. Saturation solubility was tested in 5 mL of 0.1 N HCl and in phosphate buffers at pH 6.8 and 7.4. The physicochemical properties of the nanocrystals, including physical appearance, FTIR, DSC, SEM, XRD, solubility, particle size distribution, zeta potential, and in vitro drug release, were evaluated. Results and Discussion: FTIR spectroscopy confirmed drug compatibility and ruled out potential interactions with the polymers. Nine nanocrystal formulations (F1 to F9) containing pure Azelnidipine in micronized form with varying percentages of PVP and SLS stabilizers were tested. In batches F1 to F3, the drug-to-polymer PVPK30 ratio was 1:1, and the SLS concentration was increased by 0.05, 0.10, and 0.150, yielding the highest drug release in batch F3 (97.68%). The study found that as SLS concentration increased, solubility increased; similarly, as particle size decreased, solubility increased. Conclusion: Conversion of the micronized form of Azelnidipine to the nanocrystal form increases its solubility
In vitro antioxidant and antidiabetic potential of Cinnamomum tamala and Cinnamomum verum extracts
Get PDFBackground: Diabetes is a chronic disorder characterized by oxidative stress, insulin resistance, and β-cell dysfunction. Bioactive substances found in plants, such as phenolics and flavonoids, restore redox balance and inhibit enzymes that degrade carbohydrates. Cinnamomum tamala (Buch.-Ham.) T.Nees and C.H.Eberm. and Cinnamomum verum J. Presl were used in the treatment of metabolic diseases, although less is known about their antioxidant and antidiabetic effects. Methodology: Ethanolic extracts of C. tamala leaves and C. verum bark were prepared and fractionated with polar and non-polar solvents. Phytochemical screening, total phenolic content (TPC, mg GAE/g), and total flavonoid content (TFC, mg QE/g) were measured, along with the antioxidant activity using DPPH and NO radical scavenging assays, and antidiabetic potential using α-amylase and α-glucosidase inhibition assays, using acarbose as the benchmark. Result and Discussion: Alkaloids, phenols, tannins, flavonoids, and saponins were present in both species. The n-butanol fraction had the highest TPC (16.48 mg GAE/g) and TFC (28.74 mg QE/g) in C. verum. In antioxidant assays, the ethyl acetate fraction exhibited higher radical-scavenging activity than the other solvent fractions. In C. verum, ethyl acetate fractions exhibited the strongest antidiabetic effects, with α-glucosidase inhibition comparable to that of acarbose. Both plant species exhibited significant in vitro antioxidant and antidiabetic activities. Conclusion: This study supports the use of C. tamala and C. verum in diabetes care and suggests that the ethyl acetate fraction exhibits higher in vitro antioxidant and antidiabetic activity; however, further in vivo studies, mechanistic studies, and formulation development are required to validate these findings
Salicin in modern drug discovery: A comprehensive review of pharmacokinetics, ethnopharmacology, and clinical applications
Get PDFBackground: Salicin, a prominent phenolic glycoside derived from Salix species, has traditionally been used to manage pain and inflammatory conditions. Despite its long-standing ethnomedicinal use, comprehensive knowledge regarding its pharmacokinetics, bioavailability, analytical characterization, and clinical potential remains limited. This review aims to consolidate current knowledge on salicin, encompassing its botanical sources, ethnopharmacological relevance, pharmacokinetics and bioavailability, analytical methodologies, and clinical evidence. Methods: A thorough literature search was performed using PubMed, Scopus, Web of Science, and Google Scholar. Studies reporting on salicin’s chemistry, traditional uses, pharmacological mechanisms, bioavailability, analytical profiling, and clinical trials were included. Relevant data were critically appraised and synthesized to provide an integrated overview. Results and Findings: Salix species are the primary sources of salicin, and ethnomedicinal evidence supports their use for musculoskeletal and inflammatory disorders. Pharmacokinetic studies indicate that formulation and gut microbiota significantly influence bioavailability, with rapid hydrolysis to saligenin followed by metabolism to salicylic acid. Advances in analytical methods, including spectroscopic techniques, LC-MS, and HPLC, enable precise quantification and standardization. Although large-scale, long-term trials are lacking, existing clinical studies demonstrate notable anti-inflammatory and analgesic effects with a favourable safety profile. Conclusion: Salicin holds considerable therapeutic promise, bridging traditional knowledge and modern pharmacology. Future studies should improve bioavailability, standardize analyses, and conduct robust clinical trials to confirm dosing, efficacy, and safety
Formulation, physicochemical characterizations, and stability profiling of palbociclib-loaded polymeric nanoparticle with antioxidant and anti-inflammatory investigation for breast cancer treatment
Get PDFBackground: Breast cancer is a highly prevalent malignancy worldwide with significant mortality, and conventional chemotherapy is often constrained by poor solubility, non-targeted distribution, and systemic toxicity, necessitating improved therapeutic approaches. Methodology: Palbociclib-loaded nanoparticles were formulated using chitosan, PVA, and sodium tripolyphosphate, characterized physicochemically, and evaluated for compatibility, bioactivity, stability, and MCF-7 cytotoxicity via MTT assay. Results and Discussion: PNs loaded with Palbociclib showed λmax at 342 nm, which was significantly linear between the range of 5−40 µg/ml (R² = 0.997). The particle size was 237.8 ± 1.76 nm, the PDI was 0.221, and the zeta potential was +34.09 ± 3.38 mV. The encapsulation efficiency and drug loading were 81.21 ± 1.80% and 43.0 ± 1.64%, respectively. The release was more sustained at pH 5.4 (93.25 ± 0.95%) than at pH 7.4 (80.78 ± 1.51%) after 24 h (p < 0.0001). The antioxidant activity (DPPH IC₅₀ = 0.52 µg/ml) and anti-inflammatory activity (IC₅₀ = 38.9 µg/ml) were better than free palbociclib (2.041 and 137.87 µg/ml). There was no significant change in the size (240.14 ± 1.91 nm), the PDI 0.283, the zeta potential +30.01 ± 2.68 mV, the loading of the drug (40.1 ± 1.58%), and the entrapment efficiency (79.02 ± 2.69%) after three months. PB-PNs resulted in a more pronounced proliferation inhibition effect in MCF-7 cells (IC₅₀ = 5.85 µg/ml) as compared to the free palbociclib (18.15 µg/ml).Conclusion: The developed PB-PNs constitute a stable, pH-responsive, and enhanced anticancer therapy, meriting further in vivo investigation
Design and evaluation of amphotericin b and luliconazole nanoemulsions for targeted antifungal delivery
Get PDFBackground: Drugs like Amphotericin B and Luliconazole, which are poorly soluble in water and undergo significant first-pass metabolism, often show low bioavailability. Using nanoemulsion-based delivery systems can enhance absorption and efficacy in the treatment of fungal infections. This study aimed to develop and optimize nanoemulsion formulations of Amphotericin B and Luliconazole to improve their solubility and stability and to demonstrate potential for enhanced bioavailability. Methods: Preliminary characterization of Amphotericin B and Luliconazole included solubility analysis in various solvents, melting point determination, particle size, zeta potential, FTIR spectroscopy, DSC, and XRD. Amphotericin B was further evaluated using a validated RP-HPLC method and subjected to forced degradation studies. Pseudo-ternary phase diagrams were constructed to identify suitable Smix ratios for nanoemulsion formation. Formulations were prepared by homogenization and optimized using a central composite design. Key variables included globule size, zeta potential, homogenization speed, and time. Results and Discussion: The optimized Amphotericin B nanoemulsion (NE-02-8) exhibited a globule size of 168.2 nm, zeta potential of –28.9 mV, PDI of 0.578, drug content of 99.28%, and 99.48% transmittance. Statistical optimization using a Central Composite Design (CCD) confirmed that homogenization speed and time significantly influenced globule size (p < 0.05) and zeta potential (p < 0.05). In contrast, the Luliconazole nanoemulsion showed a globule size of 327.5 nm and a zeta potential of –27.9 mV. Conclusion: Nanoemulsion formulations of Amphotericin B and Luliconazole demonstrated enhanced solubility, stability, and physicochemical properties, indicating their potential to improve drug solubilization and stability relative to conventional formulations
Formulation and optimization of simvastatin loaded nanostructured lipid carriers using central composite design
Get PDFBackground: This study aimed to formulate and optimize simvastatin-loaded nanostructured lipid carriers using central composite design. The concentrations of stearic acid, olive oil, and surfactant were designated as independent variables. The dependent variables nominated were particle size, zeta potential, and % entrapment efficiency. Methodology: Simvastatin-loaded nanostructured lipid carriers were prepared using the solvent-injection method. Polynomial equations were used to forecast the quantifiable impact of independent factors at various levels on response variables. It was found that the curvature effect was substantial and that the model was nonlinear. To optimize, the study employed the central composite design. Results & Discussions: Studies using DSC and FT-IR showed that the drug and excipients were compatible. The particle size, polydispersity index, and zeta potential values of all formulations were within the range of 133.8-460.7 nm, 0.215-0.460, and -28.3 to -32.1, respectively. The study's outcomes confirmed that olive oil significantly affects particle size and % entrapment efficiency. The relationships between the independent variables and the dependent variables were elucidated using contour plots. The experimental results and the model's predicted values were reasonably close; the statistical model can be considered mathematically valid. Conclusion: The outcomes confirmed the efficacy of the proposed design for developing simvastatin-loaded nanostructured lipid carriers with optimized properties
Cardioprotective effects of Anthocephalus cadamba bark extract and pyridoxine in STZ-induced diabetic rats
Get PDFBackground: Oxidative stress driven by hyperglycaemia and hyperlipidaemia plays a major role in diabetic cardiomyopathy. Although Anthocephalus cadamba bark and pyridoxine have traditional uses, their combined efficacy against diabetic cardiomyopathy remains underexplored. In this work, streptozotocin (STZ)-induced type 2 diabetic rats were used to investigate the preventive benefits of an ethanolic bark extract of A. cadamba given either with or without pyridoxine. Methods: Diabetes was induced in Wistar rats with STZ (45 mg/kg, i.p.). Animals were allocated to eight groups and treated with metformin, A. cadamba extract (200 or 400 mg/kg), pyridoxine (100 mg/kg), or combinations of these agents for eight weeks. Biochemical markers (CK-MB, LDH, AST), lipid profile, and oxidative stress enzymes were assessed, along with heart histopathology. Results: Diabetic rats showed marked elevations in CK-MB, LDH, and AST, which were significantly reduced by A. cadamba (200–400 mg/kg) (e.g., CK-MB, LDH, and AST decreased by approximately 25-33%). (p < 0.001). Combining pyridoxine with other therapies produced the strongest effect, lowering CK-MB, LDH, and AST by 30–41% (p < 0.001). Treatment with A. cadamba extract alone and in combination with pyridoxine significantly improved dyslipidaemia, with HDL rising from ~42 to 52% (p < 0.01-0.001) and decreasing serum-lipoproteins concentration (total Cholesterol, triglyceride, LDL, and VLDL) by ~40 to 55% (p < 0.01). Antioxidant defenses were also restored, with SOD, CAT, and GSH levels rising by 70–80% (p < 0.05–0.001). Histology confirmed reduced necrosis and fibre degeneration, most notably in the combination-treated groups. Conclusion: A. cadamba extract and pyridoxine, particularly in combination, mitigate oxidative stress, hyperlipidaemia, and cardiac injury in STZ-induced diabetic rats, suggesting therapeutic potential against diabetic cardiomyopathy
Antioxidant and hepatoprotective activity of Nigella sativa alcoholic extract in a CCl4-induced rat
Get PDFBackground: This study investigated the antioxidant, hepatoprotective, and sedative modulatory effects of Nigella sativa alcoholic extract (NSAE) in CCl4-induced hepatotoxicity in rats. Methods: Male Wistar rats were divided into six groups (n=6): normal control, CCl4 control, silymarin (50 mg/kg), and NSAE (100, 200, and 400 mg/kg). Hepatoprotective effects were evaluated through biochemical parameters, oxidative stress markers, and histopathological examination. Results: NSAE treatment (400 mg/kg) significantly restored liver function markers, including SGOT (20.95 ± 0.52 IU/L, p = 0.033) and SGPT (28.61 ± 0.67 IU/L, p < 0.001), compared to CCl4 control. Total protein and albumin levels were normalized to 5.68 ± 0.54 mg/dL and 3.84 ± 0.48 mg/dL, respectively. Antioxidant parameters showed marked improvement with NSAE (400 mg/kg), increasing GSH (0.26 ± 0.029 µmol/mg) and CAT (30.19 ± 2.69 µg/mL) while reducing MDA (0.048 ± 0.008 µg/mL). Histopathological examination revealed significant protection against CCl4-induced hepatic and gastric tissue damage, particularly at the 400 mg/kg. Conclusion: NSAE exhibited marked hepatoprotective activity comparable to silymarin, predominantly through antioxidant mechanisms and the maintenance of hepatic tissue integrity, indicating its potential as a natural therapeutic agent for managing liver diseases. Because of its hepatoprotective and antioxidant properties, NSAE may be explored in clinical settings as a natural supplement to traditional liver disease therapies or as a prophylactic for people at risk of liver disorders
Evaluation of antimicrobial and cytotoxic activities of commercial Lactobacillus acidophilus against foodborne pathogens and the MCF-7 cell line
Get PDFBackground: Lactobacillus acidophilus, a key member of the lactic acid bacteria (LAB) group, contributes significantly to both human and animal health by enhancing the microbiome. This study explores the bioactive compounds produced by L. acidophilus isolated from the Synkromax probiotic, with a focus on their antimicrobial, antifungal, and anticancer properties. Methodology: The cell-free supernatant (CFS) of L. acidophilus was subjected to solvent extraction to isolate secondary metabolites, while peptides, including bacteriocins, were partially purified using ammonium sulfate precipitation. Metabolite profiling was conducted using Gas Chromatography-Mass Spectrometry (GC-MS/MS), and Thin Layer Chromatography (TLC) was used for qualitative analysis. The antimicrobial and antifungal activities of the extracts were evaluated using the well diffusion method against pathogens, including Escherichia coli, Staphylococcus aureus, Klebsiella pneumoniae, Aspergillus niger, and Aspergillus flavus. The cytotoxic potential of the partially purified bacteriocin extract (PPBE) was assessed using the MTT assay on MCF-7 breast cancer cells. Results and Discussion: GC-MS/MS analysis identified a diverse range of bioactive secondary metabolites. Both CFS and partially purified peptides demonstrated significant antimicrobial and antifungal activity. The PPBE also exhibited strong cytotoxicity against MCF-7 cells, with an IC₅₀ value of 72.3991 µg/mL, indicating promising anticancer potential. Conclusion: Lactobacillus acidophilus from Synkromax produces a variety of bioactive compounds with potent antimicrobial, antifungal, and anticancer activities. These findings support its potential application in therapeutic development and enhancing food safety