Influence of Critical Parameters of Nanosuspension Formulation on the Permeability of a Poorly Soluble Drug through the Skin—A Case Study

Abstract

Abstract. In transdermal drug delivery systems, it is always a challenge to achieve stable and prolonged high permeation rates across the skin since the concentrations of the drug dissolved in the matrix have to be high in order to maintain zero order release kinetics. Several attempts have been reported to improve the permeability of poorly soluble drug compounds using supersaturated systems. However, due to thermodynamic challenges, there was a high tendency for the drug to nucleate immediately after formulating or even during storage. The present study focuses on the efficiency of nanoparticles and influence of different concentrations of solubilizer such as vitamin E TPGS (D-a-tocopheryl polyethylene glycol 1000 succinate) to improve the permeation rate through the skin. Effects of several formulation factors were studied on the nanosuspension systems using ibuprofen as a model drug. The overall permeation enhancement process through the skin was influenced mostly by the solubilizer and also by the size of nanoparticles. The gel formulation developed with vitamin E TPGS+HPMC nanosuspension, consequently represent a promising approach aiming to improve the permeability performance of a poorly water soluble drug candidate.

Novel nanosized formulations of two diclofenac acid polymorphs to improve topical bioavailability

“…Until now, the use of nanocrystals for dermal applications has not been intensively studied and only a few articles regarding this topic have been published (Ghosh and Michniak-Kohn, 2013;Lai et al, 2013;Romero et al, 2014;Zhai et al, 2014a). However, this technology could be very effective for improving dermal bioavailability of lipophilic substances with good skin permeability, such as DCF acid.…”

QbD Based Approach to Enhance the In-Vivo Bioavailability of Ethinyl Estradiol in Sprague-Dawley Rats

“…The area under the curve (AUC) is a vital PK parameter that explains the circulation and exposure time of the drug in bloodstreams. 43 The AUC 0-t of EENPS and EEA-QD were 20777.18 ng/mL*h and 12290.12 ng/mL*h, respectively. These increase in AUC indicated that the EE These suggested that the dissolution profile of lyophilized EENPs were distinctly superior as compared to EE.…”

Emerging role of nanosuspensions in drug delivery systems

“…The performance of ibuprofen nanosuspension and effect of varying concentrations of the solubilizer, Vitamin E TPGS to increase the permeation rate across the skin has been investigated. It was found that the entire transdermal permeation across the skin was mainly dictated by the size of nanoparticles and concentration of solubilizer [20].…”