skin permeation

Solid lipid nanoparticles (SLNs) are very potential formulations for topical delivery of antifungal drugs. The main objective for this investigation is to develop and optimize the SLNs of Acitretin for the effective topical delivery. Acitretin loaded SLNs were prepared by hot homogenization followed by the ultra sonication using Taguchi’s design and based on the results further investigation was made using central composite design (CCD). The lipid Dynasan-116, surfactant poloxomer-188 and co surfactant egg lecithin resulted in better percent drug loading and evaluated for particle size, zeta potential, TEM, drug entrapment efficiency, in vitro drug release and stability. All parameters were found to be in an acceptable range. In vitro drug release of optimized SLN formulation (F2) was found to be 95.63±1.52%, whereas pure drug release was 30.12 after 60 min. The optimized formulation was incorporated into the gel. The drug content of Acitretin gel formulation was found to 99.86 ± 0.012% and the diameter of gel formulation was 6.9 ± 0.021 cm and that of marketed gel was found to be 5.7 ± 0.06 cm, indicating better spreadability of SLN based gel formulation. The viscosity of gel formulation at 5 rpm was found to be 6.1 x 103± 0.4 x 103 cp. The release rate (flux) of Acitretin across the membrane and excised skin differs significantly. It is assumed that SLN based gel due to its appropriate physicochemical properties, high skin permeation ability, higher accumulative uptake in skin and improved skin tolerability may be more suitable as a novel regime for topical administration of Acitretin. This topically oriented SLN based gel formulation could be useful in providing site-specific dermal treatment of psoriasis with minimal drug systemic availability and high skin tolerability.

Drug delivery of highly lipophilic molecules through the transdermal route is unsuitable when systemic effect is desired. Besides the different physical and chemical approaches for permeation enhancement, a novel method has been drawn for improvement in permeation behaviour. Here, the drug molecule was supramolecularly complexed with a phospholipid molecule to form a novel chemical entity possessing improved permeation behaviour suitable for transdermal application. Curcumin (CMN) was used as model drug for preparation of Curcumin-Phospholipid Supramolecular Complex (CPSC) and was characterized by FT-IR Spectroscopy and X-Ray Diffraction Analysis. Comparative solubility study of CPSC in water and n-octanol was performed. The prepared CPSC was incorporated in polymeric matrix films of Eudragit RL100 and Eudragit RS100 and the physicochemical compatibility was studied. The permeation kinetics and permeation parameters of the films were studied against a control batch formulation loaded with uncomplexed CMN across processed excised pig ear epidermis. Skin irritation test was perfomed on rats for safety assessment of films. Analytical reports suggested supramolecular complex formation. The solubility study showed increased hydrophilicity of the prepared CPSC. The FT-IR Spectroscopy and Differential Scanning Calorimetry (DSC) confirmed no interaction between polymers and CPSC. The formulations loaded with CPSC followed zero order and Higuchi model kinetics and possessed improved permeation parameters and a good enhancement ratio against the control batch. No skin reactions were observed during the skin irritation test. The conducted experiments suggested the supramolecular phospholipid complexation to be an effective permeation enhancement technique for transdermal route.