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Anti-Infective Agents

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ISSN (Print): 2211-3525
ISSN (Online): 2211-3533

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Research Article

The Development and Evaluation of Linalool-loaded Liposomal Gel for Oral Candida Infections: Characterization, Skin Permeation, Dermal Retention, and In Vitro Anti-microbial Studies

Author(s): Vineet Kumar Rai*, Pragati Thakran, Tushar Kanti Rajwar, Alok Sharma, Kuldeep Singh Yadav, Biswakanth Kar, Goutam Ghosh and Goutam Rath

Volume 21, Issue 5, 2023

Published on: 11 September, 2023

Article ID: e090823219593 Pages: 11

DOI: 10.2174/2211352521666230809144537

Price: $65

Abstract

Background: Linalool is a known anti-fungal molecule. It could be a good candidate against oropharyngeal candidiasis if its retention in deeper skin layers, specifically at body temperature, can be extended for a long duration.

Aim: We aimed to develop and evaluate a linalool liposome-based mucoadhesive gel.

Objective: The objective of this study is to improvise localization in oral mucosa by achieving sustained release, ensuring less volatility of linalool and less permeability into the systemic circulation through the mucosa.

Methods: The liposomes were prepared by film formation and hydration method and characterized for particle size, polydispersity index, encapsulation efficiency, and morphological characteristics. The lipid carriers were dispersed into the gel matrix of carbopol 934 and HPMC.

Results: The gel was characterized and evaluated for in vitro drug release, ex vivo drug permeation through the goat mucosa and ex vivo dermal retention studies. The particle size and entrapment efficiency were 201 nm and 79.8%, respectively, with 0.300 PDI. Transmission Electron Microscopy revealed the spherical shape of the particles with a well-identified surface. The gel pH (6.8) was close to oral mucosal pH and had desired adhesiveness and rheological properties. The latter portrayed a slow linalool release (74.75% in 12 hours), low permeation (28.80% in 24 hours) through the mucosa and high retention (45%) compared to simple linalool gel, ensuring its improvised anti-microbial effectiveness against Candida.

Conclusion: A mucoadhesive liposomal gel offers a suitable medium for ensuring modified release, improved mucosal retention, and the ability to achieve the desired therapeutic effectiveness locally in mucosa for other drugs of volatile nature.

Keywords: Linalool, drug delivery, liposomes, mucoadhesive liposomal gel, skin permeation, in vitro drug.

Graphical Abstract

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