Abstract
The present study is to formulate and evaluate Acyclovir (ACV) microspheres using natural polymers like chitosan and sodium alginate. ACV is a DNA polymerase inhibitor used in treating herpes simplex virus infection and zoster varicella infections. Acyclovir is a suitable candidate for sustained-release (SR) administration as a result of its dosage regimen twice or thrice a day and relatively short plasma half-life (approximately 2 to 4 hours). Microspheres of ACV were prepared by an ionic dilution method using chitosan and sodium alginate as polymers. The prepared ACV microspheres were then subjected to FTIR, SEM, particle size, % yield, entrapment efficiency, in vitro dissolution studies and release kinetics mechanism. The FTIR spectra’s revealed that, there was no interaction between polymer and ACV. ACV microspheres were spherical in nature, which was confirmed by SEM. The particle size of microspheres was in the range of 23.8µm to 39.4µm. 72.9% drug entrapment efficiency was obtained in the formulation F3 (1:3 ratio) with a high concentration of calcium chloride (4% w/v). The in vitro performance of ACV microspheres showed sustained release depending on the polymer concentration and concentration of calcium chloride. The release data was best fitted with zero order kinetics and Korsemeyer -Peppas release mechanism and diffusion exponent ‘n’ value of was found to be Non-Fickian.
Highlights
Acyclovir is a guanosine analog that acts as an antimetabolite
The prepared ACV microspheres were subjected to FTIR, Scanning electron microscopy (SEM), particle size, % yield, entrapment efficiency, in vitro dissolution studies and release kinetics mechanism
ACV microspheres were spherical in nature, which was confirmed by SEM
Summary
Acyclovir is a guanosine analog that acts as an antimetabolite. Acyclovir is converted by viral thymidine kinase to acyclovir mono phosphate, which is converted by host cell kinases to acyclovir tri phosphate (ACVTP).ACV-TP, in turn, competitively inhibits and inactivates HSV-specified DNA polymerases preventing further viral DNA synthesis without affecting the normal cellular processes. BCS class III drug is widely used in the treatment of herpes simplex virus infection as well as varicella zoster infection. ACV is a guanosine analogue antiviral drug. It is the one of the most commonly used antiviral drug [1]. It has short biological half-life (2-4 hours) and is usually administered orally times a day. Sodium alginate and Chitosan were employed as biodegradable polymers [3, 4]
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