Chitosan-solid lipid nanoparticles as carriers for topical delivery of tretinoin

Tretinoin (TRE) or all-trans retinoic acid is employed in the topical treatment of various skin diseases including acne and psoriasis. However, its use is strongly limited by side effects and high chemical instability. TRE encapsulation in nanostructured systems reduces these problems. Chitosan is a biopolymer that exhibits a number of interesting properties such as bioadhesion and antibacterial activity. The aim of this work was to prepare and characterize solid lipid nanoparticles (SLN) containing TRE, with and without addition of chitosan, to assess their in vitro cytotoxicity in keratinocytes and to evaluate their antibacterial activity against bacteria related to acne. SLN without (SLN-TRE) and with (SLN-chitosan-TRE) chitosan were prepared by hot high pressure homogenization. The hydrodynamic mean diameter and zeta potential were 162.7 ± 1.4 nm and −31.9 ± 2.0 mV for SLN-TRE, and 284.8 ± 15.0 nm and 55.9 ± 3.1 mV for SLN-chitosan-TRE. The SLN-chitosan-TRE exhibited high encapsulation efficiency, high physical stability in the tested period (one year), were not cytotoxic to keratinocytes and showed high antibacterial activity against P. acnes and S. aureus. Therefore chitosan-SLN can be good candidates to encapsulate TRE and to increase its therapeutic efficacy in the topical treatment of acne.

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► Tretinoin is employed in the topical treatment of various skin diseases.
► The tretinoin application is limited due to the side effects and its instability.
► Tretinoin was encapsulated in solid lipid nanoparticles-chitosan (chitosan-SLN).
► The chitosan-SLN exhibited high encapsulation efficiency for tretinoin and high physical stability.
► Nanoparticles were not cytotoxic to keratinocytes and showed an important antibacterial activity against bacteria involved in the acne.