Identification of aqueous reservoirs in poly(alkylcyanoacrylate) nanoparticles

Abstract

Poly (n-butylcyanocrylate) nanocapsules were obtained by interfacial polymerization from a water-in-oil microemulsion. The latter was composed of pharmaceutically acceptable excipients such as Labrafac lipophile WL 1349 (oil), Plurol oleique CC497 (surfactant), Labrasol (co-surfactant) and was able to incorporate 20% aqueous phase. Pure n-butyl cyanoacrylate monomer (without any dilution in a halogenated solvent) was added to the microemulsion in order to obtain an oily suspension of biocompatible and biodegradable aqueous core nanocapsules. So, we provided a method of synthesis which allowed to increase by a large amount the quantity of nanocapsules synthesized at once. Finally, in order to provide a direct evidence of the presence of the aqueous core within the nanocapsules, a mass balance and nuclear magnetic resonance analysis were performed. The results showed the presence of water and Transmission Electronic Microscopy confirmed a hybrid structure of the final nanosystem, between a genuine nanocapsule and a matrix system: a nanosystem with multicavities filled with water.

Approaches to minimize the effects of P‐glycoprotein in drug transport: A review

“…Pharmaceutical/formation excipients enhanced the drug potency by inhibiting the drug metabolic pathway or transporter proteins (Veeravalli et al, 2020). Now a day, several surfactants and many natural and synthetic polymeric excipients (Table 2) are used in pharmaceutical formulation as well as in novel drug delivery systems to overcome the effects of P‐gp and deliver the therapeutic agents at the targeted place (Jeganathan et al, 2020; Thomas et al, 2020; Katekar et al, 2020; Mokhtar et al, 2019; Sulheim et al, 2016; Zhang et al, 2017; Liu et al, 2017; Watkins et al, 2017; Valicherla et al, 2016; Hoosain et al, 2015; Constantinides & Wasan, 2007; Veeravalli et al, 2020; Jacob et al, 2020). Berberine (benzylisoquinoline alkaloid) C max , AUC and relative oral bioavailability (404%) enhanced when loaded in Brij‐S20‐modified nanocrystal formulation (Xiong et al, 2018).…”