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Abstract
This study evaluates the ability of the terpenes incorporated in liposomes on the in vitro skin delivery of hydrophobic model drug, nimesulide (NE). To this purpose, so-called terpene liposomes (TPs), which are composed of phospholipid and three types of terpene, citral, limonene and cineole. The obtained formulations were characterized in terms of size distribution, zeta potential and morphology. The efficiency of TPs on skin delivery of NE was studied using in vitro Franz diffusion cells and abdominal rat skin in comparison with conventional liposomes and ethanolic solutions of NE. Results showed that all the used TPs had spherical structures with negative zeta potential, low polydispersity (PDI < 0.2), nanometric size range (z-average no more than 150 nm). TPs improved the entrapment efficiency (EE%) and gave good physical stability. In vitro skin permeation data showed that TPs were able to give a significant improvement of NE permeation through the rat skin in comparison with conventional liposomes and drug solution. Moreover, the TPs prepared with limonene were also able to deliver a higher amount of NE than the other formulation, thus suggesting that NE delivery to the skin was strictly correlated to type of terpenes incorporated liposomes. Key words: Nimesulide, terpene liposomes, in vitro skin permeation.
Highlights
The liposomes have been studied as a system for dermal and transdermal delivery (Verma and Fahr, 2004; Biruss and Valenta, 2007; Knudsen et al, 2011)
The flask was connected to a rotor evaporator under vacuum (Rotavapor, Büchi, Germany) and immersed in a water bath preheated at temperature equal or more than the transition temperature of phospholipids, in the case of lipoid S75 is about 45°C
The results showed that the average size of terpene liposomes containing citral (NE-TP1) was 194.1 with a polydispersity index (PDI) of 0.261 while the average size of the terpene liposomes containing limonene (NE-TP2) was 216.4 nm, with a PDI of 0.174
Summary
The liposomes have been studied as a system for dermal and transdermal delivery (Verma and Fahr, 2004; Biruss and Valenta, 2007; Knudsen et al, 2011). The possible mechanisms by which conventional liposomes could increase skin delivery of drugs have been appraised. These include the vesicles intact with the skin surface and its components entering the intercellular lipid matrix of the stratum corneum (SC), modifying the lipid lamellae (Kirjavainen et al, 1996). Another mechanism reported that intact vesicles might penetrate the SC, due to the effect of transepidermal osmotic pressure (Cevc and Blume, 1992). Only localized or rarely transdermal effects of tradional liposomes have been observed
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