Nanomedicine I: In vitro and in vivo evaluation of paclitaxel loaded poly-(ε-caprolactone), poly (dl-lactide-co-glycolide) and poly (dl-lactic acid) matrix nanoparticles in wistar rats

Progress in nanoscience and nanotechnology laid foundation for nanotherapy-based approach in cancer drug delivery for improved therapy and quality of life. The prepared polymeric nanoparticles (PNPs), PCL, PLGA and PLA NPs help in delivering paclitaxel (TAX) in vivo by avoiding the use of unsafe excipient, Cremophore EL. The classy microscopic examination SEM, TEM and AFM analysis revealed the spherical and smooth structure of the NPs as well as their homogeneous solid matrix without any amorphous arrangements. The FTIR analysis of PNPs exposed that there was no chemical interaction between polymer, stabilizer and TAX. The 1H NMR and XRD analyses illustrate molecular dispersion of TAX in the polymeric matrix and no evidence was observed for the presence of crystalline TAX. The outcome of in vivo acute toxicity study endorses residual solvent free PNPs. The PNPs demonstrate excellent control in delivering TAX up to 48 h with best fitted to First-order, Baker-Lonsdale, Higuchi and Korsmeyer-Peppas model. The log plasma concentration–time profile shows that the prepared PNPs were safe and have much less side-effects. The pharmacokinetic study results illustrate increase in mean residence time as result of long circulating nature of the prepared nanoparticles, which helps them to reach target area. The estimated pharmacokinetic parameters AUC0–∞ (ng h)/mL, AUMC0–∞ (ng h2)/mL, C max (ng/mL), t 1/2 (h), MRT (h), Cl (L/h/kg), V ss (L/kg) and V z (L/kg) shows improved therapeutic efficacy when compared with TAX solution.