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ISSN 2063-5346
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Preparation and Evaluation of Tableted Microcapsules of Acyclovir for Oral Controlled Release

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Ishwar Chandra Giri, Santosh Kumar Singh
» doi: 10.31838/ecb/2023.12.sa1.118

Abstract

The most popular medication for infections like cutaneous herpes, genital herpes, chicken pox, and varicella zoster is acyclovir [9-(2-hydroxyethoxymethyl)guanine], a synthetic purine nucleoside analogue derived from guanine. It is thought to be the first agent to be licenced for the treatment of herpes simplex virus (HSV-1, HSV-2) infections. The bioavailability of acyclovir is only 20%. Its elimination half-life is 2-3 hours, and it proceeds through hepatic metabolism. Hence, creating a prolonged release mucoadhesive formulation is one method by which this might be overcome. By employing the polymers Sodium Alginate, Sod CMC, HPMC K4M, and Carbopol 940, the mucoadhesive microcapsules of Acyclovir (F1-F16) were successfully synthesized by the Emulsion Solvent Evaporation method. Studies using FTIR did not find any notable medication interactions. Scan-electron microscopy showed that the produced microcapsules had acceptable spherical geometry and a smooth surface. Acyclovir mucoadhesive microcapsules were discovered to have an average particle size between 289 and 399 micrometres. In terms of percentage yield (97.6%), entrapment efficiency (87.50.32%), mucoadhesion test (703.32%), and swelling index (74.62.24%), formulation F16 was chosen as the best formulation. After 12 hours, the in-vitro drug release (F16) was discovered to be (98.120.24%). The Higuchi mechanism and Zero order kinetics were used in the formulation F16. The improved formulation F16 was kept at high temperatures, such as 250°C and 400°C, respectively, for three months. Acyclovir mucoadhesive microspheres were made into tablets using the improved formulation F16. Acyclovir mucoadhesive microcapsules and optimized acyclovir mucoadhesive microcapsules were compared in dissolving trials, and after 12 hours, the percentage of drug release was found to be 98.120.24% and 91.70.54%, respectively. The formulation F1 acyclovir microcapsules tableted was determined to be the best formulation among all formulations and can be used in the treatment of herpes simplex virus (HSV-1, HSV-2) infections based on all the aforementioned evaluation criteria.

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