Formulation and Evaluation of Acyclovir by Quality and Design based on Microsponges
Abstract
Objective: The proposed study is focussed at developing acyclovir microsponges for oral drug delivery systems. QbD was applied for better understanding of the process and to generate design space, using quality target product profile, critical quality attributes, and risk assessment. The aim of the experiment is to prepare a safe, efficacious, stable and patient compliant microsponge dosage form of Acyclovir.
Materials and methods: Pre-formulation studies were carried out which helped in developing a suitable dosage form. UV, FTIR, DSC, and SEM studies were done for pre-formulation and post-formulation evaluations. QbD was applied to generate design space, using QTPP, CQA, and risk assessment. Microsponges of acyclovir were developed by 23 factorial designs. Three variables Drug: Polymer ratio (X1), Concentration of surfactant (X2) and Stirring speed (RPM) (X3) at two levels low and high were selected and response surface plots were generated. The microsponges were prepared by Quassiemulsion solvent diffusion method. Various characterizations that were carried out include entrapment efficiency, percentage yield, particle size determination, in-vitro drug release studies and kinetic modelling of drug release. Statistical analyses of batches and surface response studies were done to understand the effect of various independent variables on the dependent variables.
Results and Discussions: The λmax was confirmed at 251 nm by UV spectroscopy. The melting point was determined experimentally to be 2460C which confirms the drug to be Acyclovir. FTIR and DSC studies confirmed that the drug is Acyclovir. Eight trials were taken as per the by 23 factorial designs.
Conclusion: The study indicates that microsponges of Acyclovir by QbD approach were successfully developed.
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Introduction
Acyclovir is a potent, specific antiviral drug which is active against herpes simplex viruses’ types I and II and varicella zoster virus [1]. Literature studies indicate that the oral bioavailability of acyclovir is relatively less, which is around 20-30%. Hence there is a need for enhancement of oral bioavailability of the acyclovir drug by employing various approaches. Acyclovir is available as various dosage forms in the market which includes capsules, creams, ointments, tablets and suspension. For all oral dosage forms the limiting factor of bioavailability which is poor. In order to overcome this limitation of oral delivery of Acyclovir, attempts have to be made to develop novel drug delivery systems of the same drug. The underlying aim of the proposed investigation is to augment the oral bioavailability of acyclovir by developing a microsponge drug delivery system of acyclovir which will attempt to increase the oral bioavailability of the drug. Microsponges are spherical small structures having large void spaces where there can be entrapment of the drug.
Conclusion
The focus of the current study was to develop microsponge drug delivery system of acyclovir using QbD approach. . Literature studies indicate that the oral bioavailability of acyclovir is relatively less, which is around 20-30%. The underlying objective of the proposed investigation is to augment the oral bioavailability of acyclovir by developing a microsponge drug delivery system of acyclovir. Preformulation studies were carried out which helped in developing a suitable dosage form. UV, FTIR, DSC, and SEM studies were done for pre-formulation and post-formulation evaluations. QbD was applied to generate design space, using QTPP, CQA, and risk assessment. Microsponges of acyclovir were developed by 23 factorial designs. Three variables Drug: Polymer ratio (X1), Concentration of surfactant (X2) and Stirring speed (RPM) (X3) at two levels low and high were selected and response surface plots were generated. The microsponges were prepared by Quassi-emulsion solvent diffusion method. Various characterizations that were carried out include entrapment efficiency, percentage yield, particle size determination, in-vitro drug release studies and kinetic modeling of drug release.