Hierarchical Porous Carbon—PLLA and PLGA Hybrid Nanoparticles for Intranasal Delivery of Galantamine for Alzheimer’s Disease Therapy

Abstract

In the present study, poly(l-lactic acid) (PLLA) and poly(lactide-co-glycolide) (PLGA) hybrid nanoparticles were developed for intranasal delivery of galantamine, a drug used in severe to moderate cases of Alzheimer's disease. Galantamine (GAL) was adsorbed first in hierarchical porous carbon (HPC). Formulations were characterized by FT-IR, which showed hydrogen bond formation between GAL and HPC. Furthermore, GAL became amorphous after adsorption, as confirmed by XRD and differential scanning calorimetry (DSC) studies. GAL was quantified to be 21.5% w/w by TGA study. Adsorbed GAL was nanoencapsulated in PLLA and PLGA, and prepared nanoparticles were characterized by several techniques. Their sizes varied between 182 and 394 nm, with an exception that was observed in nanoparticles that were prepared by PLLA and adsorbed GAL that was found to be 1302 nm in size. DSC thermographs showed that GAL was present in its crystalline state in nanoparticles before its adsorption to HPC, while it remained in its amorphous phase after its adsorption in the prepared nanoparticles. It was found that the polymers controlled the release of GAL both when it was encapsulated alone and when it was adsorbed on HPC. Lastly, PLGA hybrid nanoparticles were intranasally-administered in healthy, adult, male Wistar rats. Administration led to successful delivery to the hippocampus, the brain area that is primarily and severely harmed in Alzheimer's disease, just a few hours after a single dose.

Dissolution Enhancement and Controlled Release of Paclitaxel Drug via a Hybrid Nanocarrier Based on mPEG-PCL Amphiphilic Copolymer and Fe-BTC Porous Metal-Organic Framework

“…The average size and zeta potential of prepared nanoparticles were measured by DLS and the results are shown in Table 2 . As can be seen, prepared nanoparticles with neat paclitaxel showed sizes of about 138 nm, a value close to the ones obtained by the same technique and similar aliphatic polyesters used [ 6 , 27 , 46 ]. This value was increased to 143 nm for nanoparticles prepared with paclitaxel adsorbed to the Fe-BTC, meaning that its incorporation resulted in slightly larger-sized nanoparticles.…”

Drug Delivery With Carbon-Based Nanomaterials as Versatile Nanocarriers: Progress and Prospects

“…They can cross the BBB due to the smaller size and able to repair or heal neurons (Henna et al, 2020). Galantamine was adsorbed on the surface of hierarchical porous carbon (HPC) which was further incorporated into the poly (L-lactic acid) and poly (lactideco-glycolide) to form hybrid nanoparticles (Nanaki et al, 2020). In an animal experiment, this material successfully delivered to the hippocampus, the brain area.…”

Biodistribution of etoposide via intratumoral chemotherapy with etoposide-loaded implants

“…PLLA is a biocompatible, biodegradable synthetic polymer which has been safely used in clinical applications for over 30 years including dissolvable sutures, intrabone implants and soft-tissue implants (Fitzgerald et al., 2018 ). Furthermore, PLLA has been used as polymer matrices in the drug delivery systems (Nanaki et al., 2020 ; Ramesh et al., 2020 ). PEG4000, the other excipient in the VP16 implants was used as lubricant.…”