Abstract
The aim of the present study was to investigate transfersomes as a transdermal delivery system for the poorly soluble drug, sertraline, in order to overcome the troubles associated with its oral delivery. Different transfersomal formulations were prepared with non-ionic surfactant (span 80), soya lecithin, and carbopol 940 by the rotary evaporation sonication method. The prepared formulations were characterized for light microscopy, particle size analysis, drug entrapment, turbidity, drug content, rheological studies, in vitro release, ex vivo permeation, and stability studies. The optimized formulation was evaluated for in vivo studies using the modified forced swim model test. FTIR studies showed compatibility of the drug with excipients. The result revealed that sertraline in all of the formulations was successfully entrapped with uniform drug content. Transfersomal gel containing 1.6% of the drug and 20% of span 80 was concluded to be the optimized formulation (EL-SP4), as it showed maximum drug entrapment (90.4±0.15%) and cumulative percent drug release(73.8%). The ex vivo permeation profile of EL-SP4 was compared with the transfersomal suspension, control gel, and drug solution. The transfersomal gel showed a significantly higher (p<0.05) cumulative amount of drug permeation and flux along with lower lag time than the drug solution and drug gel. It also owed to better applicability due to the higher viscosity imparted by the gel rather than the transfersomal suspension, and no skin irritation was observed. The modified forced swim test in mice revealed that the transfersomal gel had better antidepressant activity as compared to the control gel. Thus, the study substantiated that the transfersomal gel can be used as a feasible alternative to the conventional formulations of sertraline with advanced permeation characteristics for transdermal application.
Highlights
Depression is one of the most common psychiatric disorders and is characterized by feelings of intense sadness, helplessness, worthlessness, and impaired functioning [1]
Various problems are associated with its oral delivery such as extensive first-pass metabolism, gastrointestinal disturbances such as nausea, dry mouth, diarrhea, decreased appetite etc., and its poor bioavailability (40–45%), which required this drug to be taken in high doses in order to maintain adequate plasma levels [2]
The results indicate that the process employed to prepare the transfersomes was capable of producing formulations with consistent drug content
Summary
Depression is one of the most common psychiatric disorders and is characterized by feelings of intense sadness, helplessness, worthlessness, and impaired functioning [1]. Various problems are associated with its oral delivery such as extensive first-pass metabolism, gastrointestinal disturbances such as nausea, dry mouth, diarrhea, decreased appetite etc., and its poor bioavailability (40–45%), which required this drug to be taken in high doses in order to maintain adequate plasma levels [2]. Vesicular systems have been widely explored as surrogate vehicles for topical and transdermal drug delivery. Their benefits in enhancing drug permeation have been well established [4]. Despite the strong rationale for the use of vesicles in transdermal drug delivery, the major problem in the development of vesicular systems at industrial and clinical levels is their poor stability
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