Ibuprofen Loaded Electrospun Polymeric Nanofibers: A Strategy to Improve Oral Absorption

Abstract

The poor aqueous solubility of candidate drugs has presented a great challenge to formulation scientists for their effective oral delivery. Poor solubility is often associated with poor dissolution behavior and, subsequently, poor bioavailability for those drugs when intestinal absorption is dissolution rate limited. In the present study electrospun polymeric nanofibers were developed to address the poor aqueous solubility of ibuprofen, a Biopharmaceutic Classification System (BCS) class-II drug. Hydrophilic spinnable polymers like polyvinyl pyrrolidone were deployed as a carrier system for the fabrication of nanofibers. The electrospinning parameters like flow rate, voltage, and spinneret to collector distance were optimized. The fabricated ibuprofen-loaded nanofibers were characterized using scanning electron microscopy and differential scanning calorimetry. Drug release studies and ex vivo intestinal absorption studies were also carried out. The nanofiber-based platform significantly improved in vitro absorption of ibuprofen compared to pure ibuprofen crystals.

Optimal delivery of poorly soluble drugs using electrospun nanofiber technology: Challenges, state of the art, and future directions

“…Solid state characterization revealed no crystalline traces indicating the amorphous state of ibuprofen in the fabricated nanofibers. In another study to improve the oral absorption of ibuprofen, hydrophilic matrix former like PVP K30 was used to fabricate nanofibers via electrospinning method (Panda et al, 2022). The electrospinning method adopted and the matrix forming polymer was responsible for amorphization of ibuprofen in the loaded nanofibers which eventually improved the in vitro dissolution and ex vivo intestinal permeation of the drug.…”

“…Though suspension electrospinning has evolved as an approach where the solubility of component ingredients may be compromised, this approach has less contribution towards the development of nanofibers for solubility enhancement of poorly soluble drugs. Dissolution of therapeutic agents from nanofibers can be improved when the drug and polymers are molecularly dispersed, the drug particles' size is reduced to nano or micro scale, and the drug exists in an amorphous state (Panda et al, 2022). Hence, the solubilizing capacity of solvents is to be considered carefully while choosing solvents for electrospinning applications.…”

“…Drug‐loaded matrix type nanofibers may be fabricated using a simple conventional type single needle electrospinning equipment (Panda et al, 2022). The working fluid typically consists of solution/dispersion of drug(s) and suitable hydrophilic polymer(s).…”

“…These intriguing techniques encompass chemical modification (Mallick et al, 2007; Takahashi et al, 2020), co‐crystals (Nechipadappu et al, 2017; Teoh et al, 2020), micro/nanonization (Pattnaik, Swain, Manaswini, Divyavani, et al, 2015; Pattnaik, Swain, Rao, Varun, & Subudhi, 2015), polymorphic ameliorations (Liu et al, 2015), lipid‐based systems (Castro & Lindqvist, 2020; Rahman et al, 2019), micellar solubilization which includes self‐emulsifying drug delivery systems (Chou et al, 2020; Yang et al, 2019), inclusion complexes (Mahapatra et al, 2013), amorphous solid dispersion/solution (Guo et al, 2021; Smeets et al, 2018), etc. Nanotechnology has additionally contributed nicely to seeking solutions for improved solubility and/or bioavailability of drug substances (Panda et al, 2022; Pattnaik, Swain, Manaswini, Divyavani, et al, 2015; Pattnaik, Swain, Rao, Varun, & Subudhi, 2015). Among all such available techniques, the strategies involving developing amorphous solid drug products have received lots of momentum within the recent past because of the vast improvement of solubility of candidate drugs following this approach.…”

“…The electrospun nanofibers have several biomedical applications including drug delivery, gene delivery, tissue engineering, biosensing, etc. (Keirouz et al, 2020; Krysiak & Stachewicz, 2022; Panda et al, 2022; McCullen et al, 2009).…”