Transfersomes: A Novel Vesicular Carrier for Enhanced Transdermal Delivery of Sertraline: Development, Characterization, and Performance Evaluation

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.

Betamethasone Dipropionate Gel for Treatment of Localized Plaque Psoriasis

“…It was reported that at high surfactant concentration, the drug release was low due to formation of rigid micelles [45]. These findings were agreed with Shaji et al [48] and Gupta et al [29], who reported that drug release was related to EE and drug loading. In the present study the optimum surfactant concentration for drug release was found to be achieved by using 5 mg tween 80.…”

“…In the present study the optimum surfactant concentration for drug release was found to be achieved by using 5 mg tween 80. This finding is also agreed with Gupta et al [29], and Kaylani et al [49], who found that the use of tween 80 as a non-ionic surfactant significantly increased (p<.0.05) drug release from the transfersomal suspensions compared with SDC as an ionic surfactant. The possible explanation of the enhancing effect of tween 80 on drug release rate was the large volume of hydrophilic head group consisting of several polyethylene chains [50].…”

“…The changes in the percentage of BD content during the six months were statistically insignificant (p>0.05) indicating good chemical stability. Many studies reported good chemical stability at refrigerated condition (4 °C) and at room temperature (25 °C) [19,25,26,29,51,52].…”

“…The stability of BD loaded transfersomes was evaluated after storage for 6 mo at 4 °C and 25 °C by studying the change in the organoleptic characters, drug content (chemical stability) and in vitro drug release (physical stability) [19,[22][23][24][25][26][27][28][29].…”

Advancing the Pharmaceutical Potential of Bioinorganic Hybrid Lipid‐Based Assemblies

“…However, these bilayer and acyl‐chain lipid products have not fulfilled their practical potential due to their insufficient morphological stability and inclusion leakage in vitro and in vivo 9. To address these drawbacks, various optimizations have been approached,10 which include surface coating with certain amphiphilic molecules (PEGylation; where PEG is polyethylene glycol) and cholesterols for prolonging circulation,11 enhancing elasticity using transferosome formulations for transdermal delivery,12 and improving bioavailability that employ drug–lipid conjugates 13. Although these strategies have significantly promoted the therapeutic potential of traditional lipid nanoparticles with increasingly broad applications, several concerns such as insufficient coverage of surface coating on phospholipid bilayers,14 and the morphological stability of lipid assemblies are likely to decrease after modulating composition, charge, and bilayer architecture.…”