Posted by admin on May 31, 2021 in |
The objective of the present study was to improve the oral bioavailability using high-density gastro-retentive pellets containing solid dispersion of acyclovir. Solid dispersion prepared with polyvinylpyrrolidone (PVP K30) and hydroxypropyl methylcellulose (HPMC) using different ratios 1:1, 1:2, 1:3, 1:4, and 1:5 by solvent evaporation method and characterized for solubility study, dissolution study, FT-IR, DSC, and XRD. High-density gastro-retentive pellets containing solid dispersion of acyclovir was prepared by extrusion/spheronization technique using solid dispersion of acyclovir with PVP K30 (1:3), Barium sulphate as high-density material, microcrystalline cellulose (MCC) as extrusion aid, ethylcellulose (EC) as release retarding polymer and HPMC as swellable gel-forming polymer. The formulation was optimized based on in-vitro release profile and characterized for pellets morphology, micro-meritics properties, FT-IR, DSC, XRD, and in-vivo study. The optimized formulation F8f showed the release for 12 h with an increase in retention at the absorption site. Release kinetic studies of optimized formulation showed that the data best fit in Higuchi’s model. The in-vivo studies like pharmacokinetic parameters and X-ray transmission were investigated in...
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Posted by admin on May 31, 2021 in |
Benzoxazole and its analogues play an important role as therapeutic agents and exhibit good cytotoxic as well as antimicrobial activity. In the present study, benzoxazole analogues have been prepared by synthetic route; their spectroscopic evaluation was carried out, and then the synthesized compounds were screened for their cytotoxic activity by Allium cepa root model as well as antimicrobial activity by cup plate method. The synthesis and cytotoxic activity of a novel series of Schiff’s base was carried out by reacting the amino group of the 4-Benzoxazol-2-yl-phenylamine with different aromatic/ heteroaromatic aldehydes in the presence of polyphosphoric acid to give 4-(1,3-Benzoxazol-2-yl)phenyl]-1-(Substituted phenyl) methanimine (4a-4h) also Diazotization reaction of (4-Benzoxazol-2-yl phenyl) with β napthol gave 2-((4-(benzo [d]oxazole-2-yl)phenyl) diazenyl) naphthalene-2-ol (4i). The cytotoxic and antimicrobial activities of the synthesized compounds were determined by using the onion root model and cup plate method, respectively. The activity data of compounds was compared with standard drugs Cefixime for antibacterial activity and miconazole for antifungal was used as a standard, and cyclophosphamide was used as a...
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Posted by admin on May 31, 2021 in |
Plants are the important constituents of folk and traditional medicines and fulfill nutrition and dietary needs from ancient times. The aim of this study to evaluate phytochemicals and antioxidant activity of seed oil of wild apricot (Prunus armeniaca L). Thenon-cultivated seed of wild Prunus armeniaca L. from the Garhwal, Uttarakhand, India was analyzed for its phytochemicals e.g., total phenols, tannins, and total alkaloids by Folin-Ciocalteau reagent, Folin-Denis reagent, and solvent extraction method, respectively. Antioxidant activity of seed oil was determined by DPPH, reducing power assay and nitric oxide scavenging method. Results obtained showed that seeds of P. armeniaca contain tannins (6.47 %), total phenols (0.27%), a total alkaloid (0.22 %). P. armeniaca seed oil showed significant antioxidant activity when analyzed by DPPH, reducing power assay, and nitric oxide free radical scavenging method. Moreover, the IC50 value of seed oil from DPPH, reducing power and nitric oxide assays were 0.1, 0.5, and 0.5 mg/ml and % scavenging activity range 24.12-84.82% respectively. These studies clearly show that P. armeniaca seed oil...
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Posted by admin on May 31, 2021 in |
In the present study, 3-naphthoyl propionic acid and various appropriate reagents were used to synthesize, ten new synthetic furanone derivatives, i.e. 3-arylidene-5-(naphthalen-2-yl) furan-2(3H)-one (2-11). Selected furanones were made to react with ammonia and benzylamine to yield analogous pyrrolones (12-16) and N-benzyl pyrrolones (17-21), respectively, which were characterized on the basis of 1H NMR, Mass spectroscopic data. Synthesized compounds were tested for anti-inflammatory activity by the carrageenan-induced rat paw edema method, compounds displaying compelling anti-inflammatory activity were screened for analgesic activity by employing the acetic-acid induced writhing method, and selected compounds were tested for ulcerogenic activity. Screening of the newly synthesized compounds was also done for their antibacterial profile against Escherichia coli, Staphylococcus aureus, Pseudomonas aeruginosa, and antifungal activity against Aspergillus flavus, Aspergillus niger. One of the derivatives numbered (9) displayed strong anti-inflammatory, analgesic, and antimicrobial activities, and it could prove as a promising candidate for the development of new and safer...
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Posted by admin on May 31, 2021 in |
The present work aims to formulation and characterization of a topical liposomal gel for ciprofloxacin hydrochloride. The drug lipid interaction studies were carried out by FTIR analysis, X-ray diffraction study, and DSC study, and no changes of physicochemical properties of ciprofloxacin were found. The thin-film hydration method was used for the preparation of liposomes consisting of phosphatidylcholine (PC) and cholesterol (CH). For hydrogel preparation, Carbopol 940 was used. The maximum entrapment efficiency of 79.51 ± 2.395 was found from liposomes formulated with PC/CH at a weight ratio of 30:10 (batch number – F5), and by increasing cholesterol content above this limit, the encapsulation efficiency decreased. All the prepared formulations were found stable and the liposomal gel approach of ciprofloxacin hydrochloride showed better skin residential time than the marketed formulation. The in-vitro drug permeation was found to be around within the range of 0.194-0.319 over a period of 12 h for different batches. In conclusion, ciprofloxacin hydrochloride liposomal hydrogel is a smart and suitable drug delivery system for improving the...
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