Journal of Applied Pharmaceutical Research (JOAPR)
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Antimicrobial potential, GC-MS analysis, and molecular docking studies of Pogostemon benghalensis leaf extract
Get PDFBackground: Pogostemon benghalensis has several medicinal uses in Northeast India, including wound healing activity. Currently, no molecular modeling research has examined the antimicrobial potential of its phytoconstituents. This molecular docking research identifies bioactive chemicals and evaluates their antibacterial properties. Methodology: Phytochemical screening and in vitro antibacterial tests were performed on a crude ethyl acetate extract of Pogostemon benghalensis leaves. After GC-MS analysis revealed the phytoconstituents, in-silico molecular docking was performed against the dihydrofolate reductase (DHFR) enzymes of Escherichia coli and Staphylococcus aureus. Results and discussion: The crude ethyl acetate extract of Pogostemon benghalensis leaves included alkaloids, carbohydrates, flavonoids, glycosides, tannins, and phenolic compounds. The extract also demonstrated potent in vitro antibacterial activity against E. coli and S. aureus. GC-MS data demonstrated that Phytol was the most abundant compound (53.72%) followed by Oxirane, dodecyl (13.51%.). Molecular docking studies demonstrated identified compounds have high binding affinity (BA) to the bacterial DHFR enzyme. Notable compounds are Androst-5-ene-3,19-diol, 3-acetate (3 β) with -7.4 kcal/mol BA against E. coli DHFR and -10.1kcal/mol against S. aureus DHFR; Retinol acetate with -8.7 kcal/mol BA against E. coli DHFR and Phytol with -6.5 kcal/mol BA against E. coli DHFR and -6.7 kcal/mol BA for S. aureus DHFR respectively. Conclusion: The results show that Pogostemon benghalensis contains valuable bioactive compounds with high antibacterial activity which further validates the use of this plant as a wound healing medication. However, further in vivo experimental validation of these results and their toxicological implications are required
A bioanalytical method development and validation for quantification of glycopyrrolate and neostigmine in rat plasma by LC-MS and its application to pharmacokinetic study
Get PDFBackground: After surgery, non-depolarizing neuromuscular blocking medications include neostigmine (NEO) and glycopyrrolate (GLY). Numerous traditional approaches, such as HPLC and UPLC procedures, are established for the quantification of GLY and NEO; nevertheless, they lack sensitive and specific analysis, especially in complex matrices. Using the LC/MS approach, this work develops a bioanalytical method for quantifying both drugs in rat plasma and applies it to pharmacokinetic studies. Methodology: The plasma was extracted using acetonitrile, and Rivastigmine was employed as an internal standard. An MRM method with positive ions was used for multiple reactions. A C18 column and a mobile phase - 70:30 mixture of acetonitrile and buffer was utilised at a flow rate of 1 ml/min. Plasma vortex for 10 minutes and centrifuged at 4000 rpm at 20°C. Validation and stability studies are conducted according to the ICH guidelines. The pharmacokinetic study by WinNonlin (Version 5.2) software. Results and Discussion: Rt for Glycopyrrolate and Neostigmine at 1.838 and 2.800min. GLY has a precision (%CV) of 0.45 at HQC and 3.57 at LQC. NEO had a precision (%CV) of 1.13 at HQC and 2.79 at LQC. From 2 to 40 ng/mL of GLY and 10 to 200 ng/mL of NEO, the standard curves showed a linear relationship. LOD and LOQ for both drugs were 3pg/mL and 10pg/mL. Conclusion: A simple, affordable, reliable, and sensitive approach for quantifying GLY and NEO in rat plasma using LC-MS, with Rivastigmine serving as the internal standard, was developed, validated, and successfully applied in the pharmacokinetic study of rat plasma
A study on design & development of betamethasone acetate and betamethasone sodium phosphate extended-release suspension
Get PDFBackground: The development of an injectable composition of betamethasone sodium phosphate and betamethasone acetate with an equivalent drug release profile to the marketed reference drug product, "Celestone Soluspan®," is highly challenging. To overcome this drug development problem, there is a need for a practical methodology for the preparation and evaluation of injectable compositions. Methodology: Different sterilization methods (Dry Heat Sterilization and Autoclave) and phase methods (two- or three-phase methods) are used for the preparation of the injectable composition of betamethasone sodium phosphate and betamethasone acetate. Two-phase or three phase methods and order of addition of excipients during the preparation of the formulation are the unique methodology of the present study and plays an important role in the stability of the composition. The release profile of the developed formulations is determined by using a USP type IV dissolution apparatus (STF buffer pH 7.4 as dissolution medium, 6.0 ml/min flow rate for 120 min), and stability study is also performed. Results and Discussion: As per the results of the present study Trial no. 3 shows betamethasone freebase 2.68% and total impurities 3.52% at 40°C /75% RH for 90 days and also gives similar release profile (f2 value 95%) as compared to the marketed formulation/RLD (Reference Listed Drug) i.e. Celestone Soluspan®. Conclusion: Present study concludes that injectable suspension of betamethasone sodium phosphate and betamethasone acetate using dry heat sterilisation of betamethasone acetate and three-phase method shows superior results or equivalent release profile as compared to the RLD and the key features of the present study
Development of a fast-acting nanosuspension nasal drop using a novel co-processed polymer for migraine relief
Get PDFBackground: Effective central nervous system (CNS) drug delivery remains challenging due to the blood-brain barrier. Nasal drug delivery offers a non-invasive alternative, ensuring rapid drug absorption and onset of action. Prochlorperazine Maleate, a drug for migraines, suffers from poor solubility, limiting its therapeutic potential. Methodology: A nanosuspension-based nasal drop was developed and optimized using high-pressure homogenization. A novel co-processed polymer enhances solubility and stability. Key formulation parameters, including particle size, zeta potential, and polymer concentration, were optimized using a central composite design. The optimized nanosuspension was characterized for its physicochemical properties, drug release, and stability. Results and Discussion: The optimized formulation (Batch F9) exhibited a particle size of 78.8 nm and a high drug release rate (93.87% in 8 hours). Stability studies confirmed no significant changes in drug content, pH, or osmolality over a three-month period. The nasal drop provided consistent dosing, with each actuation delivering a precise amount of drug content. In vitro drug release studies demonstrated a sustained release pattern, enabling prolonged migraine relief. Conclusion: The developed nanosuspension nasal drop presents a promising solution for CNS drug delivery, ensuring rapid and sustained therapeutic outcomes. This nanosuspension nasal drop achieved a 5.6-fold enhancement in solubility and demonstrated rapid onset within 10 minutes post-administration. Although promising, the study is limited to in vitro characterization; future research should explore in vivo efficacy and long-term safety
Preliminary phytochemical screening, FT-IR, and HPTLC analysis, and antioxidant, antimicrobial activities of methanolic extracts of Dalbergia sisso leaves
Get PDFBackground: Dalbergia sissoo is a well-known plant known as Shisham. It has medicinal importance, including analgesic, antipyretic, and antiemetic properties. Therefore, the primary objective of this research is to investigate the bioactive constituents in the methanolic leaf extract of Dalbergia sisso by characterizing it using FT-IR and HPTLC techniques, and to determine its antioxidant and antimicrobial activities. Methodology: A Soxhlet apparatus was used for the extraction process. 150 g of Dalbergia sisso powdered leaves was extracted using a Soxhlet apparatus for 30 hours, utilizing methanol as a solvent. The solvent was vaporized and concentrated to produce a dry residue once the extraction was finished. The yield percentages for the methanolic extract were 4.8% respectively. Result and Discussion: FT-IR spectroscopy showed different peak values for functional compounds in the methanolic extract. The FTIR spectrum of the methanolic leaf extract shows the interpretation of the chemical bonds in the methanolic leaf extract. HPTLC studies revealed that the active compound lupeol is present in the methanolic extract. Conclusion: It has been concluded that the methanolic extract of Dalbergia sisso leaves contains lupeol and quercetin bioactive compounds. The methanolic extract of Dalbergia sisso leaves was found to have antioxidant and antimicrobial effects. The HPTLC technique found lupeol, which may possess antioxidant and antimicrobial activities. The FT-IR spectrum revealed the presence of hydroxyl, hydrocarbon, aldehyde, allene, and secondary alcohol groups in the methanolic extract, consistent with the presence of quercetin. The methanolic leaf extracts show the presence of saponin, alkaloids, flavonoids, anthraquinone glycosides, and tannins
Niosomes: an extensive analysis of its structure, preparation, and uses in drug delivery
Get PDFBackground: Niosomes are sophisticated drug delivery vehicles composed of non-ionic surfactants that have a lot of potential for delivering drugs. Their unique bilayer structure enables the targeted and regulated release of both fat-soluble and water-soluble medications, enhancing their stability and absorption. This review discusses the components, production processes, benefits, drawbacks, and potential uses of niosomes in various medical fields, including cutaneous medication delivery and cancer treatment. Objective: This article provides an in-depth overview of niosomes as novel drug delivery vehicles, highlighting their benefits, preparation techniques, applications, and assessment criteria. It aims to highlight how they can improve therapeutic efficacy and bioavailability across various medicinal domains. Methodology: This article outlines multiple techniques employed in the preparation of niosomes, including the ether injection method, sonication method, hand-shaking method, extrusion method, thin film hydration, microfluidization method, and Transmembrane pH gradient drug uptake process. It also examines elements that impact niosome synthesis, such as the kind of surfactant utilized, the drug's characteristics, and environmental conditions. Conclusion: Ongoing research is focused on enhancing niosomal formulations and expanding their use in clinical settings, despite challenges such as instability and a short shelf life. Overall, niosomes are a significant development in drug delivery technology, with the potential to enhance treatment effectiveness and improve patient care
Phytochemical profiling and antioxidant assessment of Cassia auriculata leaves via GC-MS
Get PDFBackground: This research aimed to investigate the phytochemical composition, quantify key bioactive compounds such as phenolics and flavonoids, analyze the secondary metabolite profile using GC-MS on methanolic leaf extracts, and evaluate the antioxidant capacity via the DPPH assay. Methodology: The Soxhlet extraction method is employed to obtain crude extracts of Cassia auriculata using solvents including ethanol, methanol, chloroform, and water. These extracts undertook qualitative analysis to detect various bioactive phytochemicals. The total phenolic and flavonoid concentrations were quantified. The methanolic leaf extract underwent phytochemical analysis using a gas chromatography-mass spectrometry (GC-MS) device, following established procedures. The antioxidant capacity of the methanolic leaf extracts was assessed by determining their ability to scavenge free radicals of 2,2-diphenyl-1-picrylhydrazyl. Results and Discussion: Initial phytochemical screening revealed the presence of various secondary metabolite groups. Out of all the solvent extracts assessed, the methanolic extract displayed the highest concentrations of phenolic and flavonoid compounds, measuring 9.48 ± 0.06 mg of Gallic acid equivalents per gram of extract and 6.56 ± 0.03 mg of Quercetin equivalents per gram of extract, respectively. GC-MS analysis of the methanolic extract identified 28 bioactive compounds with known pharmacological significance. Conclusion: The antioxidant activity, evaluated using the DPPH radical scavenging assay, demonstrated that the methanolic extract had the most potent radical scavenging effect among the extracts tested (IC50-48.96 µg/ml). These findings suggest that Cassia auriculata leaves extract is a promising source of natural antioxidants and bioactive compounds, supporting its traditional use in herbal medicine
Development and evaluation of non-saccharide polymer-based taste-masked clarithromycin tablets: a novel approach to improve pediatric compliance
Get PDFBackground: Clarithromycin, a macrolide antibiotic, is commonly prescribed for respiratory and skin infections. However, its intensely bitter taste significantly hampers patient compliance, especially in pediatric and geriatric populations. The present study focused on formulating a novel taste-masked clarithromycin tablet using non-saccharide polymers to improve palatability while maintaining pharmacological performance. Methodology: Taste masking was accomplished by employing Eudragit E-100, Ethyl Cellulose, and Hydroxypropyl-β-Cyclodextrin (HP-β-CD) as coating agents. Granules were formulated using a bottom-spray fluidized bed coating process, followed by compression into tablets. These were assessed for physical parameters, disintegration time, in vitro drug release, and sensory evaluation using an electronic tongue system. The dissolution behavior was compared with that of a marketed clarithromycin formulation. Stability testing was conducted under accelerated (40°C/75% RH) and long-term (25°C/60% RH) storage conditions. Result and Discussion: The optimized formulation (Batch B9) demonstrated complete taste masking, exhibiting a bitterness score of 0 on the electronic tongue. Sensory data projected an over 85% improvement in patient acceptability. The tablets disintegrated within 60 seconds and showed a drug release of 98.1% within 30 minutes. Comparative dissolution profiling indicated no statistically significant difference (p > 0.05) between the test and reference products. Stability studies confirmed robust physicochemical stability for six months under both storage conditions. Conclusion: The study successfully developed a taste-masked clarithromycin tablet employing non-saccharide polymers, ensuring effective taste masking, rapid disintegration, and consistent drug release. This formulation offers a promising approach to enhance treatment compliance, particularly in populations sensitive to taste
Development of expeditious RP-HPLC method for simultaneous estimation of bilastine and montelukast in fixed dosage combination
Get PDFBackground: Bilastine and montelukast are used to treat allergic rhinitis and chronic urticaria. Due to the recent increase in highly allergic disorders, demand for this combination has risen. Therefore, for regular quality control analysis, a new, rapid, and cost-effective method has become crucial. Compared with the previously reported methods, the present method is ultra-fast, with well-separated peaks within ̴ 3.0min and a total run time of 8 min. Because it uses a methanol-buffer system, it is less expensive, more environmentally friendly, and safer than an acetonitrile-based method. This study presents a rapid, specific, and economical “reversed-phase high-performance liquid chromatography (RP-HPLC)” method for the simultaneous estimation of Bilastine and Montelukast. Methodology: The chromatographic conditions for the separation of drugs are achieved by leveraging a tailored composition of mobile phase with methanol and acidic phosphate buffer with a volume ratio of 55:45v/v, the “Zorbax C18 column (4.6×150mm, 5µ)” maintained at 35ºC with an optimized flow rate of 1.0 mL/min and detected at a wavelength of 260 nm. The injection volume is 10 µL, and the run time is 8 min. Results and Discussion: The retention times for the drugs bilastine and montelukast are 2.061 and 2.462 min, respectively. Linearity is observed with correlation coefficients of 0.9993 and 0.9994, respectively, for montelukast and bilastine at 1-5 µg/mL and 100-500 µg/mL. Efficient separation and quantification of these two therapeutically important compounds were achieved in this method. Conclusion: The developed analytical method has been validated in accordance with International Conference on Harmonisation (ICH) guidelines, demonstrating satisfactory performance with respect to specificity, accuracy, precision, linearity, and robustness. This novel RP-HPLC approach provides a valuable tool for pharmaceutical analysis and quality control
Phytochemical profiling and evaluation of in-vitro antidiabetic effects of Pyracantha crenulata (D. Don) M. Roem. fruit extracts
Get PDFBackground: Pyracantha crenulata (D. Don) M. Roem. is a species of flowering plant, commonly known as Nepalese or Himalayan firethorn, and belongs to the Rosaceae family. Various species of the genus Pyracantha have been reported to reveal antidiabetic activity. The literature suggests that the fruits are conventionally used to reduce blood sugar levels, warranting further research. Therefore, this research provides valuable insights into phytochemical profiling and antidiabetic potential of different extracts of Pyracantha crenulata (D. Don) M. Roem fruits with in vitro models via alpha (α)-amylase and alpha (α)-glucosidase enzyme inhibition assay. Methodology: The successive extraction of Pyracantha crenulata (D. Don) M. Roem fruit was carried out by using different solvents with increasing polarity, including n-hexane, ethyl acetate, ethanol, and distilled water (dH2O) via the Soxhlet extraction technique. The distinct unprocessed extracts were then subjected to a qualitative/quantitative phytochemical investigation of phytonutrients, followed by an assessment of their in vitro antidiabetic potential. Results and Discussion: The results concluded that phytocompounds, including flavonoids, phenols, steroids, and tannins, were tentatively identified in this plant. The extracts inhibit alpha (α)-glucosidase and alpha (α)-amylase enzymes in a dose-dependent way. Among all the extracts, the ethanolic extract exhibited potent anti-diabetic activity, with an IC50 of 44.79 µg/ml at 100 µg/ml in the α-amylase inhibitory assay and 30.09 µg/ml at 100 µg/ml in the α-glucosidase inhibitory assay, which is comparable to that of the standard acarbose. Conclusion: The study demonstrates that ethanolic fruit extract ameliorates hyperglycemia by releasing bioactive substances, providing a rationale for its traditional use as a natural hypoglycemic agent