Abstract

The objective of present study was to develop nonionic surfactant vesicles of proteolytic enzyme serratiopeptidase (SRP) by adapting reverse phase evaporation (REV) technique and to evaluate the viability of SRP niosomal gel in treating the topical inflammation. The feasibility of SRP niosomes by REV method using Span 40 and cholesterol has been successfully demonstrated in this investigation. The entrapment efficiency was found to be influenced by the molar ratio of Span 40 : cholesterol and concentration of SRP in noisome. The developed niosomes were characterized for morphology, particle size, and in vitro release. Niosomal gel was prepared by dispersing xanthan gum into optimized batch of SRP niosomes. Ex vivo permeation and in vivo anti-inflammatory efficacy of gel formulation were evaluated topically. SRP niosomes obtained were round in nanosize range. At Span 40 : cholesterol molar ratio 1 : 1 entrapment efficiency was maximum, that is, 54.82% ± 2.08, and showed consistent release pattern. Furthermore ex vivo skin permeation revealed that there was fourfold increase in a steady state flux when SRP was formulated in niosomes and a significant increase in the permeation of SRP, from SRP niosomal gel containing permeation enhancer. In vivo efficacy studies indicated that SRP niosomal gel had a comparable topical anti-inflammatory activity to that of dicolfenac gel.

Highlights

  • Recent advancements in biotechnology and genetic research have led to an increased surge of interest in the use of peptide and protein drugs

  • Results of preliminary studies revealed that the stable niosomes of SRP could be prepared using cholesterol and Span 40 by adopting reverse phase evaporation (REV) technique

  • The entrapment efficiency is the crucial parameter in the preparation niosomal formulation and formulation scientist’s efforts are always directed towards achieving high entrapment efficiency

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Summary

Introduction

Recent advancements in biotechnology and genetic research have led to an increased surge of interest in the use of peptide and protein drugs. Proteolytic enzymes represent an important class of proteins and peptides with primary pharmacological use as anti-inflammatory and digestive agents. In recent years many researchers substantiating that the vesicular structures, such as liposomes, niosomes, ethosomes, and transfersomes, are acting as the best carrier for administration of drugs across the skin. These vesicular structures act as carriers for drugs and help to overcome the barrier properties of the skin. A vesicular drug delivery system, has been used as a drug carrier or reservoir due to its intrinsic skin penetration enhancing properties and more stability than other vesicular systems like liposomes, ethosomes, and so forth. The present study is based on the hypothesis that incorporation of SRP into niosomes will improve its penetration across the skin, which will in turn improve local anti-inflammatory efficacy of SRP upon topical administration

Materials and Methods
Characterization of SRP Niosomes
In Vivo Efficacy Evaluation
Results and Discussion
Results
Conclusion
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