Abstract
Cationic nanocapsules represent a promising approach for topical delivery purposes. We elaborated on a novel formulation based on the cationic nanocapsules to enhance the pharmacodynamic efficacy, user compliance, and photostability of tretinoin (TTN). To achieve this goal, TTN nanocapsules were prepared by the nanoprecipitation method. In order to statistically optimize formulation variables, a Box-Behnken design, using Design-Expert software, was employed. Three independent variables were evaluated: total weight of the cationic acrylic polymer (X1), oil volume (X2), and TTN amount (X3). The particle size and encapsulation efficiency percent (EE%) were selected as dependent variables. The optimal formulation demonstrated spherical morphology under scanning electron microscopy (SEM), optimum particle size of 116.3 nm, and high EE% of 83.2%. TTN-loaded nanocapsules improved photostability compared to its methanolic solution. The in vitro release study data showed that tretinoin was released in a sustained manner compared to the free drug. The ex vivo skin permeation study demonstrated that greater drug deposition into the epidermal region rather than the deep skin was observed with a gel containing TTN-loaded nanocapsules than that of drug solution, respectively. The skin irritation test revealed that the nanoencapsulation of the drug decreased its irritancy compared to the free drug. These results revealed the promising potential of cationic nanocapsules for topical delivery of tretinoin
Highlights
Tretinoin (TTN) is a first-generation retinoid with keratolytic and anti-inflammatory activities which is used topically in the treatment of various dermatological diseases such as photoaging, acne, and psoriasis [1,2,3]
The nanoprecipitation method was used in which the TTN can be loaded during NC formation by evaporating the organic solvent. Solvent removal parameters such as evaporation temperature, time, and speed were selected based on the characteristics of the prepared nanocapsules and previous studies [12, 13, 31]
Lowboiling solvents such as acetone with ΔHvap of 32 kJ mol−1 or less could be completely removed under reduced pressure
Summary
Tretinoin (TTN) is a first-generation retinoid with keratolytic and anti-inflammatory activities which is used topically in the treatment of various dermatological diseases such as photoaging, acne, and psoriasis [1,2,3]. Nanocapsules are specific polymeric nanoparticles with a core-shell organization in which the polymeric wall surrounds an oily core [15]. These nanocapsules have important advantages, such as higher drug loading capacity and improved ability to protect the encapsulated drug from degradation [15, 16]. They exhibit slow and sustained release of incorporated drugs which makes them suitable for cutaneous applications [17]
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