Kinetics of Drug Release via Nicardipine Hydrochloride‐loaded Carboxymethyl Cellulose/Poly(D,L‐lactic‐co‐glycolic acid) Nanocarriers Using a Contemporary Emulsion Process

Abstract

A contemporary synthesis of polymeric nanocarriers based on drug delivery systems was employed using a water in oil in water (W 1 /O/W 2) double emulsion process to develop nicardipine hydrochloride-loaded carboxymethyl cellulose/ poly(D,L-lactic-co-glycolic acid) (NCH-CMC/PLGA) nanocarriers. The optimal synthesis of the nanocarriers was studied, including polymer amount, cross-linker concentration, and emulsifier concentration. The synthesized nanocarriers were smaller than~169 nm and showed a drug encapsulation of more than 80% and a yield of 51% to 73%. The NCH-CMC/ PLGA nanocarriers presented good stability in aqueous dispersion for 10 days. Controlled drug release from the nanocarriers was slow and continuous for up to 16 days. The nanocarriers protected the drug against degradation and maintained therapeutic drug concentrations. In addition, the transport of drug release was studied via five conventional mathematical modelings such as Zero-order model, Firstorder model, Hixson-Crowell model, Higuchi model, and Korsmeyer-Peppas model. The Korsmeyer-Peppas model was fitted to achieve mathematical modeling for the optimized formulation of nanocarriers. Moreover, significant cytocompatibility was observed at all tested doses of NCH-CMC/PLGA nanocarriers. The NCH-CMC/PLGA nanocarriers could be an effective drug delivery agent for calcium channel blockers.

Aliphatic Polyester Nanoparticles for Drug Delivery Systems

“…The strategy for controlled release is based on polymer degradation at a rate that is effective for the treatment of cerebral vasospasms for 4-14 days. However, a clinical scenario needs to be investigated in the future [6].…”

“…This absorption results from the hydrophobic properties of aliphatic polyesters and leads to surface erosion. In the next stage, an amorphous region becomes swollen followed by stress relaxation of the polymer chain [6]. Next, the matrix can absorb additional water molecules via a diffusion mechanism that leads to the hydrolysis of the polymeric chains in the matrix, creating matrix porosity.…”

“…PDLLA, with methyl groups in its structure, has reduced chain mobility (chain configuration), leading to more hydrophobicity than PGA, which is devoid of these methyl groups (Figure 1). PGA is a highly hydrophilic polymer that can absorb more water molecules [6,13]. Thus, PGA hydrolysis is more complimentary than PDLLA hydrolysis.…”

“…The T g value may impact the kinetics of drug release from delivery systems. For instance, PLGA micro/nanoparticles were prepared via the emulsion solvent evaporation method [6,7,[21][22][23]. The residual solvent was removed via evaporation to harden the nanoparticles.…”

“…Due to the short biological half-life of NCH, we were able to modify the NCH pharmacokinetics via carboxymethyl cellulose/poly(d,l-lactide-co-glycolide) (NCH-CMC/PLGA) nanoparticles using a contemporary emulsion process [6]. PLGA is an aliphatic polyester with hydrophobic properties that is highly biocompatible and biodegradable.…”