Objective:

To assess the UDL-ClAlPc permeability, retention and biodistribution in vivo.

Methods:

Transferosomas were obtained by lipid film re-hydration method. Wistar rats were treated topically and intraperitoneally with UDL-ClAlPc for 5 days. Skin and organs were collected five and thirty days after-treatment to determine ClAlPc retention and histopatho-logical studies. The ClAlPc was extracted with solvents and quantified by fluorometry. The results were expressed in nM PcAlCl/mg organ. The permeation was tested ex vivo using Franz-diffusion cells and the retention in stratum corneum and epidermis-dermis by tape stripping.

Results:

In the ex vivo experiments ClAlPc-UDL was not able to penetrate rat skin and was retained mainly in the stratum corneum. In rat, five days after topical treatment ClAlPc was retained mainly in the stratum corneum (41.76±0.02) with minimum concentrations in spleen (0.09±0.02), epidermis-dermis (0.06±0.17), liver (0.03±0.02) and lung (0.02±0.01 nM). After intra peritoneal treatment, ClAlPc was found in spleen (0.58±0.4), brain (0.07±0.07), heart (0.07±0.12), lung (0.01±0.012) and skin (0.021±0.02 nM). Thirty days post-treatment ClAlPc was not found in any organ. Histopathological studies were negative.

Conclusion:

The ClAlPc contained in transferosomes was retained mainly in the stratum corneum. Low concentration was detected in dermis a place where the parasite survives. This vehicle needs to be improved to increase skin penetration.

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