Optimizing lornoxicam-loaded poly(lactic-co-glycolic acid) and (polyethylene glycol) nanoparticles for transdermal delivery: ex vivo/in vivo inflammation evaluation

Abstract

Aim: This study focused on developing a topical gel incorporating lornoxicam-loaded poly(lactic-co-glycolic acid) and polyethylene glycol (PLGA-PEG) blend nanoparticles to mitigate gastrointestinal (GIT) side effects and enhance therapeutic efficacy.

Materials & methods: Synthesized nanoparticles were subjected to in vitro characterization, ex vivo permeation studies, and acute oral toxicity analysis post-incorporation into the gel using a S/O/W double emulsion solvent.

Results & conclusion: The nanoparticles displayed a smooth, spherical morphology (170–321 nm) with increased entrapment efficiency (96.2%). LOX exhibited a permeation rate of 70–94% from the nanoparticle-infused gel, demonstrating favorable biocompatibility at the cellular level. The formulated gel, enriched with nanoparticles, holds promising prospects for drug-delivery systems and promising improved therapeutic outcomes for LOX.

Article highlights

Utilizing the S/O/W double emulsion solvent evaporation method, LOX-loaded PLGA-PEG nanoparticles were fabricated with a sustained release effect intended for topical use.
The study evaluated the effects of dependent characteristics, such as encapsulation effectiveness, particle size, and percentage penetration of nanoparticles, on independent parameters, such as homogenization speed, and percentage of PEG and PLGA concentration.
To evaluate the drug–polymer compatibility and interactions, a variety of methodologies, including FTIR analysis, ex vivo permeation, XRD acute oral toxicity analysis, surface morphology evaluation, percentage yield, and particle size assessment, were used to characterize the nanoparticles.
A relationship between the PLGA concentration and these other responses was evident, as increasing the PLGA concentration resulted in larger nanoparticle sizes and increased encapsulation efficiency.
In contrast, the effects of homogenization speed and PEG percentage on particle size and encapsulation efficiency decreased, indicating that higher homogenization speeds and percentages of PEG produced smaller nanoparticles with lower encapsulation effectiveness.
The results of scanning electron microscopy showed smooth, spherical nanoparticles with appropriate boundaries. FTIR research confirmed that there was no drug–polymer interaction, confirming the compatibility of the components with the Carbapol 940 gel as well. Biocompatibility and safety profiling of the developed system were ensured by acute oral toxicity analysis.
Skin penetration studies have shown that higher PLGA concentrations improve the topical sustained release impact of nanoparticles, whereas higher PEG percentages and faster homogenization lead to better skin penetration rates.
As a result, gel-containing PLGA-PEG nanoparticles have become a viable option for topical medication delivery, providing advantages for improved penetration and sustained drug delivery.

Read also our introduction article on Topical Excipients here:

excipients formulation