Solubility and Dissolution Enhancement of Tadalafil Using Self-Nanoemulsifying Drug Delivery System

Abstract

The aim of this study was to develop and evaluate self-nanoemulsifying drug delivery system (SNEDDS) of tadalafil (TDL) in order to enhance its aqueous solubility and dissolution rate. TDL SNEDDS were developed by aqueous phase titration method via construction of pseudo-ternary phase diagrams. The formulations which passed thermodynamic stability and self-nanoemulsification tests were further characterized in terms of droplet size, viscosity, % transmittance and drug content. Selected SNEDDS and drug suspension were subjected to in vitro drug release studies via dialysis membrane in phosphate buffer (pH 6.8). In vitro drug release studies showed 96.6% release of TDL from optimized SNEDDS F5 as compared to only 12.4% from drug suspension after 24 h of study. The results of solubility studies showed 1434 folds enhancement in TDL solubility from optimized SNEDDS F5 as compared to its aqueous solubility. Overall, these results indicated that developed SNEDDS could be successfully used to enhance solubility and dissolution rate of poorly soluble drugs such as TDL.

Bioavailability enhancement and pharmacokinetic profile of an anticancer drug ibrutinib by self-nanoemulsifying drug delivery system

“…In this work, the value of n in all SNEDDS (I1‐I5) and IBR suspension was recorded in the range of 0.954–0.991, indicating non‐Fickian mechanism in all SNEDDS and suspension . These results were in good agreement with previously published reports on drug release kinetics of essential oil and tadalafil nanoemulsion/SNEDDS …”

Formulation, characterization, in vitro and in vivo evaluations of self-nanoemulsifying drug delivery system of luteolin

“…These are isotropic mixtures of oil, emulsifier and coemulsifier which form oil-in-water nanoemulsion when diluted with water [47]. SNEDDS are known to improve solubility, dissolution [48][49][50][51][52][53], bioavailability [54][55][56][57] and therapeutic benefits of loaded drugs [58,59].…”

Physicochemical properties of tadalafil solid dispersions – Impact of polymer on the apparent solubility and dissolution rate of tadalafil

“…Poor solubility in water is a limiting factor for its 90 absorption leading to significant differences in the pharmacologi-91 cal response. Several methods have been already investigated for 92 Td solubility enhancement including cyclodextrin complexation 93 [1], preparation of nanoparticles [16] and self-nanoemulsifying 94 drug delivery systems [4]. In our previous study the amorphous 95 form of Td was obtained using several commercially available 96 amorphization techniques [25].…”