Journal of Applied Pharmaceutical Research (JOAPR)
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In vitro antioxidant effects of hydroalcoholic extract of Cassia tora aerial part using different models
Get PDFBackground: Free radicals, harmful by-products of a cell's natural metabolism, are responsible for various health problems. The search for plant-based supplements or medicines is always in high demand, as is the antioxidant activity that contributes to the therapeutic efficacy of plants. Aim: In the present study, the hydroalcoholic extracts from the aerial parts of Cassia tora were used for in vitro analysis of their antioxidant activity. Methods: Six separate assay methods were used to evaluate the antioxidant activity, i.e., against hydroxyl radical, DPPH, superoxide anions, nitric oxide, and also total flavonoid and phenolic content, were investigated. This was done by standardizing hydroalcoholic extract (70/30 ethanol to water) of Cassia tora and ascorbic acid. Results: Percentage scavenging activity and IC50 value were measured for extract prepared at various concentrations. The results IC50 values were 25.54 µg/ml, 45.04 µg/ml, 36.56 µg/ml, and 97.61 µg/ml for DPPH, superoxide radicals, hydroxyl radicals, and nitric oxide, respectively. Subsequently, the total phenolic and flavonoid content in the extract obtained was 1.927±0.73 mg GAE/gm and 1.018±0.29 mg QE/gm, respectively. Conclusion: The hydroalcoholic extract of Cassia tora contains more phytoconstituents. This suggests it has a wide range of medicinal antioxidant properties that make it helpful in treating many diseases. With the increasing demand for safer herbal treatments, scientific efforts in this field are making significant contributions and advances and supporting innovation
Treatment with Terminalia chebula (retz.): possible mechanism of inhibition of spermatogenesis and fertility in albino mice
Get PDFBackground: There has been a continued effort to develop an effective male contraceptive of plant origin due to its ready availability, cost-effectiveness, and fewer side effects. The present study has evaluated the mechanism of inhibitory action of Terminalia chebula Retz. (T. chebula; family: Combretaceae) on spermatogenesis and fertility in albino mice after oral administration of the aqueous bark extract (100, 300, and 500 mg/kg BW daily) of T. chebula for 35 d. Methodology: The effects of the Terminalia treatment on various reproductive endpoints such as sperm parameters, testis histology, activities of 3ß- and 17ß-HSDs, immunoblot expressions of StAR and AR proteins, immunostaining of AR, serum testosterone level, LPO level, activities of SOD and catalase, and fertility indices were investigated. Toxicological and recovery studies have also been performed. Results: Testes in Terminalia-treated mice showed nonuniform histologic alterations. Sperm parameters, activities of 3ß- and 17ß-HSDs, immunoblot expressions of StAR and AR proteins, immunostaining of AR, and serum testosterone level were adversely affected, though activities of SOD and catalase were unchanged. Libido remained unaffected, but fertility was inhibited markedly in treated males without signs of toxicity. By 42 d of treatment discontinuation, Terminalia-induced deviations in the reproductive endpoints recovered to control levels. Conclusion: The results of the present study indicate that T. chebula treatment reversibly inhibits spermatogenesis and fertility without signs of toxicity. Further, antifertility effects result from diminished production of testosterone due to Terminalia-mediated inhibition of testicular steroidogenesis
An update on phytoconstituents and pharmacological importance of Asparagus racemosus
Get PDFBackground: Asparagus racemosus (family: Liliaceae), is a well-researched traditional or ancient medicine in the Siddha, Ayurveda, and Unani systems. It is commonly known as Satawar, Satamuli, Satavari, and found at low altitudes throughout India. It contains bioactive metabolites such as fructo-oligosaccharides, polysaccharides, asparosides, shatavarins, sapogenins, racemosols, isoflavones, glycosides, mucilage, and fatty acids, while saponin is one of the main active constituents of asparagus.
Objective: Across the globe, Asparagus racemosus gained importance for its ethano-pharmacological value in curing various ailments. This review will outline the medicinal properties, uses, and value addition of Asparagus racemosus.
Methods: We have reviewed and retrieved the relevant information by probing the main keywords in online databases (PubMed, Scopus, Science Direct and Web of Science, etc.). Screening of relevant abstracts/ title and full papers were done to pick the suitable content based on the pharmacological profile of Asparagus racemosus.
Conclusion: The whole plant possesses pleiotropic therapeutic activity, antioxidant, anti-inflammatory, immunomodulatory, neuroprotective, nootropic, antidepressant, etc., without showing any remarkable side effects. It also treats stomach ulcers, diabetes, kidney disorders, and Alzheimer's disease, etc
Formulation and development of bilayer tablet containing irbesartan and metformin hydrochloride for diabetic hypertensive patients
Get PDFBackground: Hypertension is a common complication of type II diabetes. The present research work aimed to develop bilayer tablets that would manage type II diabetes patients with hypertension. The prepared bilayer tablet has an immediate-release layer of anti-hypertensive irbesartan and a sustained-release (SR) layer of anti-diabetic metformin hydrochloride. The purpose of these bilayer tablets was to increase patient compliance by converting two separate monotherapy to single combination therapy. Methodology: Several ratios of polymers, including HPMC K100M, EC, Eudragit, and Guar gum, were employed to prolong the drug release for twelve hours. An immediate-release layer of irbesartan was prepared by spherical agglomeration. The physical properties, drug content, solubility profiles, release kinetics, and stability of prepared bilayer tablets were assessed. Results and Discussion: The examination of SR granules and bilayer tablets revealed outstanding packing qualities and excellent flow properties, with bulk and tapped densities ranging from 0.39-0.46 g/cm³ and 0.42-0.55 g/cm³, respectively. In vitro dissolution tests revealed that the immediate-release layer gave an initial burst of Irbesartan. Still, the sustained-release layer of metformin showed controlled drug release over 12 hours at greater polymer concentrations. According to stability testing, the bilayer tablets' physical properties, drug content, and dissolving profiles did not change significantly. Conclusion: The bilayer tablet combination of Irbesartan and Metformin exhibited desired physical features, controlled drug release, and stability. This formulation represents a viable treatment option for diabetic hypertensive patients, offering effective and consistent management of both disorders while improving patient compliance
Pharmaceutical development of etodolac transfersomal gel for topical drug delivery system in rheumatoid arthritis
Get PDFBackground: Transferosomes provide delivery of the drug into systemic circulation via the skin as a topical delivery system. So, this study started with the objective of formulating Etodolac transfersomal gel to enhance its skin permeation. Methodology: A total of nine transferosomes (ET-1 to ET-9) containing lecithin, different grades of span and tween, were successfully prepared using a rotary film evaporator. Results and Discussion: After primary evaluation, results were as particle sizes ranged from 222 to 421 nm, zeta potential shows results from –18.50 to –62.53 mV with PDI values 0.254 to 0.303, and the entrapment efficiency (EE%) of Etodolac in the transferosomes ranged from 54.15% to 80.25%. Additionally, the transfersomes formulations were included in carbopol 940 gels (ETC-1 to ETC-9 and EC-0 without transferosomes) and assessed for various characteristics like color, pH, homogeneity, spreadability, viscosity, and in vitro drug release study. Optimized formulation (ET4 and ETC4) underwent further analysis using SEM, TEM, DSC, FTIR, XRD, ex vivo skin permeation, skin irritation and in vivo studies. The in vivo results were compared. % edema inhibition maximum was observed with optimized transfersomal gel formulation (ETC4) as compared to the marketed formulation and plain Carbopol gel when the study was completed after 8 hrs. Conclusion: After this research, it is suggested that Etodolac Transfersomal gel (ETC4) can be considered as an alternate drug carriers system for topical delivery and it could be used to treat Rheumatoid Arthriti
Bioanalytical method for the simultaneous estimation of atoltivimab, maftivimab and odesivimab in rat plasma by LCMS/MS and its application to a pharmacokinetic study
Get PDFBackground: A quick, accurate, reproducible, and straightforward liquid chromatography-tandem mass spectrometry(LC-MS/MS) system employing Atoltavimab, Maftivimab, and Odesivimab as an internal standard for Zanamivir quantification was achieved. Zanamivir is a neuraminidase inhibitor that effectively treats influenza caused by influenza A and B viruses. Methodology: Whenever we use the Kinetex C-18 column, all HPLC parameters and conditions are obeyed, so we use this column. Separation was performed on a Kinetex C18 column (100 mm x 4.6 mm, 2.6µm) using isocratic elution with a buffer containing 1mL of formic acid in 1Lit of water and a mobile step consisting of a 40:60 v/v mixture of two elements, buffer and acetonitrile, with a flow rate of 1mL/min at 300C temperature was used. Results & Discussion: We used different stationary phases in the optimization process, such as C18, C8, and CN-propyl. Using a kinetex C18 column with dimensions of (100 mm x 4.6 mm, 2.6 µm) connected to a PDA detector, we obtain strong peak shapes of Atoltivimab, Maftivimab, and Odesivimab from various trials. Flow rates in the mobile process were set to 1 mL/min. Conclusion: Atoltivimab, Maftivimab, and Odesivimab analysis was completed in 7 minutes over a good linear concentration range of 5ng/mL to 100ng/mL (r2 = 0.999), 5ng/mL to 100ng/mL (r2 = 0.999), and 5ng/mL to 100ng/mL (r2 = 0.9998). The findings of the precision and recovery studies are within the appropriate range
Formulation and evaluation of phytosomes containing bioactive from Carica papaya seeds
Get PDFBackground: Papaya seeds are a rich source of proteins, fat, fibers, vitamins, minerals, monounsaturated fatty acids, polyphenols, and powerful antioxidants like flavonoids. Low solubility limits the absorption and bioavailability of herbal constituents. Hence, phytosomes of Papaya seed extract were formulated to enhance its solubility and bioavailability. Methodology: Papaya seeds were extracted using ethanol as solvent, and all the phytoconstituents present in the extract were assessed during the phytochemical screening and LC-MS analysis. In-vitro antidiabetic activity pure extract was determined by alpha-amylase and alpha-glucosidase enzyme inhibitory assay. The phytosomes of extract were formulated using the lipid thin film formation method and Soya lecithin and Cholesterol as lipids. The formulated phytosomes were analyzed for parameters such as particle size, zeta potential, encapsulation efficiency, percent drug content, and In-vitro dissolution study. The chemical nature of the formulation was studied using FTIR analysis and powder X-ray diffractometry. Thermal stability of phytosomes analyzed with the help of Differential Scanning calorimetry. Results: LC-MS identified 16 phytoconstituents. In-vitro antidiabetic activity showed 59.97% and 51.17% inhibition of enzymes alpha-amylase and alpha-glucosidase, respectively. The encapsulation efficiency of the optimized formulation was 88.41±0.91% with a particle size of 188.0±53.7nm. TEM images of formulation confirm the formation of phytosomes. FTIR, DSC, and Powder X-ray diffractometry showed no unwanted peaks. The in vitro dissolution study showed 89.26±1.05% CDR of phytosome, while the extract showed 47.78±0.59% CDR. Conclusion: Evaluation results of phytosomes suggest that this formulation can be used as an effective herbal antidiabetic formulatio
Innovative approach for improved sustained delivery of metformin hydrochloride for its anti-hyperglycemic activity
Get PDFMetformin hydrochloride, an antidiabetic agent, is useful in reducing the blood glucose concentration in Type II diabetes. It is also finding its use as a repurposed drug. The formulations consisted of micro drug delivery systems prepared by emulsification method and were evaluated in-vitro and in-vivo. Process variables like amount of polymer, speed of agitation and stirring, presence or absence of surfactant and cross linker offered a versatile approach towards obtaining the formulation though affected physicochemical properties of formulations. Discrete, spherical, and free-flowing microspheres, in the size range and granularity of 250 to 700µ were used to control the drug release rate. Drug release was diffusion controlled as evident from the Higuchi kinetics. The physical characteristics of the formulations were reproducible. Healthy and alloxan induced hyperglycaemic male albino mice were used for in-vivo experimentation by evaluating plasma glucose level reduction and % reduction in the blood glucose level after administration of pure drug and formulations. The results indicate significant sustained fall in the blood glucose level for about 10 hrs following formulation administration as compared to the pure drug
Systematic approach to develop and validate High Performance Liquid Chromatographic method for efavirenz and its degradants
Get PDFBackground: The crucial aspect to consider during method development and validation, ensuring accurate, precise, and specific estimation of drug substances and drug products, is stability. Various factors, including environmental, instrumental, reagent, and human factors, can pose challenges in achieving suitable method development and validation. Objective: This work aimed to develop and validate a low flow rate, LCMS compatible, simple, and rapid reverse-phase high-performance liquid chromatographic method for estimating efavirenz and its degradation products at different stress conditions. Materials and Methods: The HPLC system employed a Phenomenex Luna 5μ C18 (2) 100A (250 x 4.6 mm) column and a mobile phase of methanol: 20 millimolar ammonium formate solution (90:10) adjusted to pH 4 with formic acid. All analytes were separated within 15 minutes and detected at 247 nm. Method validation was carried out according to ICH guidelines, including linearity, accuracy, precision, ruggedness, robustness, LOD, and LOQ. Results and Discussion: The method was linear in the 10-90 μg/ml range, with a regression coefficient 0.999. Intra- and inter-day precisions, ruggedness, and robustness were within acceptable limits (≤2% RSD) with LOD and LOQ of 0.35 and 1.16 μg/ml, respectively. Degradation study indicates well resolution of the drug and degradants. Conclusion: Purposeful degradation of efavirenz resulted in different degradation products under various stress conditions, and the method demonstrated satisfactory resolution from its degradants
Solubility enhancement of etoricoxib using inclusion complexation with cyclodextrins: formulation of oro dispersible tablets by QbD approach
Get PDFBackground: The work was intended to enhance etoricoxib's solubility and dissolution rate and then develop oro-dispersible tablets for faster onset of action. Methodology: Inclusion complexes (ICs) of the drug were obtained with β-cyclodextrin (β-CD) and hydroxypropyl β-cyclodextrin (HP β-CD) at ratios of 1:0.125, 1:0.25, 1:0.5, 1:1, and 1:2 (w/w). The selected cyclodextrin at appropriate drug carrier proportion was used to develop oro-dispersible tablets (ODTs) by direct compression, adding crospovidone as a super disintegrant. Phase solubility studies of etoricoxib were carried out by using multiple concentrations of β-cyclodextrin and hydroxypropyl β-cyclodextrin, i.e., 1 %, 2 %, 3 % w/v in distilled water at 37±2°C. Spectroscopic (FT-IR) and thermal analysis (DSC) techniques were employed to identify the drug-carrier interactions. Result: It showed that etoricoxib solubility improves with increasing hydrophilic carrier concentration. The Gibbs free energy values (ΔG˚tr) are consistently negative, showing the solubility of etoricoxib. Significant drug carrier interaction in spectroscopic or thermal analysis was not found. Discussion: The ICs of drugs with β-CD and HP β-CD have successfully addressed the challenges of solubility enhancement and taste masking for etoricoxib. Conclusions: It is observed that the inclusion complexes formed by the kneading method using β-cyclodextrin (β-CD) at a 1:1 ratio and hydroxypropyl β-cyclodextrin (HP β-CD) at a 1:2 ratio can be used to improve dissolution. Hence β-CD (at a 1:1 ratio) is selected for the formulation of oro-dispersible tablets. ODTs offer more patient compliance and an alternative to available conventional tablets