Abstract
The study aims to investigate the propylene glycol-based liposomes named ‘proposomes’ in enhancing skin permeation of drugs with different physicochemical properties. Ibuprofen, tofacitinib citrate, rhodamine B, and lidocaine were loaded into proposomes. These drug formulations were analyzed for particle size, zeta potential, polydispersity index, entrapment efficiency, and in vitro skin permeation. The confocal laser scanning microscopy was performed on skin treated with calcein and rhodamine B laden proposomes. The transdermal delivery relative to physicochemical properties of drugs such as logP, melting point, molecular weight, solubility, etc., were analyzed. We tested the safety of the proposomes using reconstructed human skin tissue equivalents, which were fabricated in-house. We also used human cadaver skin samples as a control. The proposomes had an average diameter of 128 to 148 nm. The drug’s entrapment efficiencies were in the range of 42.9–52.7%, translating into the significant enhancement of drug permeation through the skin. The enhancement ratio was 1.4 to 4.0, and linearly correlated to logP, molecular weight, and melting point. Confocal imaging also showed higher skin permeation of calcein and rhodamine B in proposome than in solution. The proposome was found safe for skin application. The enhancement of skin delivery of drugs through proposomes was dependent on the lipophilicity of the drug. The entrapment efficiency was positively correlated with logP of the drug, which led to high drug absorption.
Highlights
Transdermal delivery has been widely studied due to its many advantages, such as avoiding first-pass metabolism, reducing side effects, improving patient compliance, and increasing bioavailability
The average size of most of the proposomes ranged from 140 to 150 nm, except for rhodamine B, which has a smaller size of 128 nm
The smaller particle size of rhodamine B proposomes could be attributed to the ion–ion interaction between the positively charged quaternary amine in rhodamine B and the negatively charged phosphate group in Soya phosphatidylcholine (SPC) [43]
Summary
Transdermal delivery has been widely studied due to its many advantages, such as avoiding first-pass metabolism, reducing side effects, improving patient compliance, and increasing bioavailability. The three ways in which a drug molecule could penetrate skin are intracellular, intercellular, and follicular pathways. Regardless of which pathway the drug takes, the major challenge in this transdermal mode of drug delivery is the presence of the outermost stratum corneum (SC), made up of corneocytes interdispersed in the lipid matrix. SC acts as a primary barrier, only allowing small and lipophilic molecules to pass through [1]. Various methods have been developed over the past few decades to enhance drug permeation through the skin [2,3].
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