EVALUATING THE IMPACT OF PREPARATION CONDITIONS AND FORMULATION ON THE ACCELERATED STABILITY OF TRETINOIN LOADED LIPOSOMES PREPARED BY HEATING METHOD
Keywords:
Heating method, Ionic strength, Liposome, Tretinoin, Zeta potential, Accelerated stabilityAbstract
Objective: The aim of this study was to prepare stable all-trans retinoic acid or tretinoin (RA) loaded liposome formulation with high encapsulation efficiency intended for immediate application on the skin using the simple preparation method.
Methods: Formulas were prepared by heating method. The effect of formulation variables on liposome properties was investigated. Dynamic Light Scattering Process (DLS) and the electrophoretic mobility process were used to determine the mean size and zeta potential, respectively. The encapsulation efficiency % was determined spectrophotometrically. Six liposome formulas (Fs) were prepared. Three types of phospholipids and two ratios of cholesterol were used. Sodium cholesteryl sulfate (SCS) was added to all formulas except formula 1. Six formulas and topical ethanolic solution of RA was stored at accelerated storage conditions for six months. EE% was determined by validated H. P. L. C method in the stage of the stability study.
Results: pH=6.5 showed the highest EE%. Substantial decrease in zeta potential and EE% was noticed by increasing the ionic strength. SCS showed a positive effect on the stability of liposomes. Hydrogenated soybean phosphatidylcholine (HSPC) showed the best results on the stability of liposomes and RA. The leakage of RA from liposomes was not observed when the cholesterol was added to the formulas.
Conclusion: The phospholipid that has a phase transition temperature (Tm) above the storage temperature showed the best stability with time and prevented the leakage of the active substance without needing to add cholesterol. It is necessary to add charge inducing substance to the formula to improve its stability.
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References
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