Development of Ultradeformable Liposomes with Fatty Acids for Enhanced Dermal Rosmarinic Acid Delivery.

Thirapit Subongkot,Praneet Opanasopit,Tanasait Ngawhirunpat

doi:10.3390/pharmaceutics13030404

Thirapit Subongkot, Praneet Opanasopit + Show 1 more

Open Access

https://doi.org/10.3390/pharmaceutics13030404

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Journal: Pharmaceutics	Publication Date: Mar 18, 2021
Citations: 13	License type: CC BY 4.0

Affiliation: Silpakorn University, Burapha University

Abstract

This study aimed to develop ultradeformable liposomes (ULs) with fatty acids, namely, oleic, linoleic, and linolenic acid, to improve the skin penetration of rosmarinic acid. This study also investigated the vesicle-skin interaction and skin penetration pathway of ULs with fatty acids using the co-localization technique of multifluorescently labeled particles. The prepared ULs were characterized in terms of size, surface charge, size distribution, shape, % entrapment efficiency (% EE), and % loading efficiency (% LE). The prepared ULs with fatty acids had an average particle size between 50.37 ± 0.3 and 59.82 ± 17.3 nm with a size distribution within an acceptable range and exhibited a negative surface charge. The average % EE and % LE were 9 and 24.02, respectively. The in vitro skin penetration study found that ULs with oleic acid could significantly increase the skin penetration of rosmarinic acid compared to ULs. According to confocal laser scanning microscopy observations, this study suggested that UL vesicles attach to the skin before releasing the entrapped drug to penetrate the skin. These findings suggested that ULs with oleic acid penetrated the skin via the transfollicular pathway as a major penetration pathway.

Highlights

IntroductionDermal drug delivery is the transportation of active compounds into the skin for various purposes, such as disease treatment as well as diagnosis and cosmetic application
The delivery of drugs into the skin is limited by the stratum corneum, which is the outermost layer of the skin
Rosmarinic acid has a molecular weight of 360.3 g/mol, log partition coefficient of 1.82, and pKa of 3.57 [4]

Summary

Introduction

Dermal drug delivery is the transportation of active compounds into the skin for various purposes, such as disease treatment as well as diagnosis and cosmetic application. The skin is the largest organ and consists of heterogeneous layers, including the epidermis, dermis, and subcutaneous tissue. The delivery of drugs into the skin is limited by the stratum corneum, which is the outermost layer of the skin. Rosmarinic acid is a polyphenolic compound that has various biological activities, such as anti-inflammatory [1], antioxidant, and antimelanogenic properties [2,3]. Due to its useful pharmacological properties, the delivery of rosmarinic acid into the skin is beneficial for skin health. Rosmarinic acid has a molecular weight of 360.3 g/mol, log partition coefficient (log P) of 1.82, and pKa of 3.57 [4]

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