Herein, lipid-polymer core-shell hybrid nanoparticles composed of poly(D,L-lactic-co-glycolic acid) (PLGA)/lecithin (PLNs) were synthesized through lipid-based surface engineering. Lipids were absorbed onto the surface of the PLGA core to enhance the advantages of polymeric nanoparticles and liposomes. The amounts of lipids and encapsulation of the drug nicardipine hydrochloride (NCH) in the PLNs were studied. NCH-loaded PLNs (NCH-PLNs) were produced in high yield (66%) with a high encapsulation efficiency (92%) and a size of 176 nm. The mass of phosphorus (P) on the NCH-PLN surface was qualitatively and quantitatively investigated using X-ray fluorescence spectroscopy, and lecithin addition increased the P mass percentage due to the phosphate group (PO43-) in its structure. These data confirmed the lipid-based surface engineering of NCH-PLNs. The zeta potential of NCH-PLN exceeded -30 mV, ensuring colloidal stability, and preventing precipitation through electrostatic stabilization. In vitro, NCH was continuously and slowly released from NCH-PLNs over 16 days. Furthermore, PSVK1 cells exhibited high viability after treatment with NCH-PLNs, indicating favorable cytocompatibility. After comparing various mathematical equations of drug release kinetics, the data best fit the Korsmeyer-Peppas model with R2 values of 0.989, 0.990, and 0.982 for 1.0, 3.0, and 5.0 mg/mL lecithin, respectively. The release exponents obtained ranged from 0.480 to 0.505, suggesting anomalous transport release. Thus, NCH-PLNs have potential as a robust drug delivery platform for the controlled administration of NCH, particularly for vasodilation during neurosurgery.
Poly(D,L-lactic-co-glycolic acid) (PLGA) is an important material used in drug delivery when controlled release is required. The purpose of this research is to design and characterize PLGA microparticles (PLGA MPs) implants for the controlled release of nicardipine hydrochloride (NCH) in vitro. This study used the water-in-oil-in-water (w1/o/w2) double emulsion and solvent diffusion/evaporation approach to prepare PLGA MPs. Optimal processing conditions were found, such as polymer content, surfactant type, stabilizer concentration, inner and outer aqueous phase volumes, and stirring speed. The PLGA MPs for use as nicardipine hydrochloride (NCH) loading and release had spherical morphology, and the average diameter was smaller than μm. The release kinetics were modeled to elucidate the possible mechanism of drug release. In vitro release studies indicated that the NCH release rate is slow and continuous. PLGA MPs are an interesting alternative drug delivery system, especially for use with NCH for biomedical applications.
Drug delivery systems using aliphatic polyester nanoparticles are usually prepared via an emulsion process. These nanoparticles can control drug release and improve pharmacokinetics. Aliphatic polyesters are linear polymers containing ester linkages, showing sensitivity to hydrolytic degradation. The byproducts then promote autocatalytic degradation. These byproducts could enter the Krebs cycle and be eliminated from the body, resulting in the high biocompatibility of these nanoparticles. The properties of these polyesters are linked to the drug release rate due to biodegradation, i.e., polymer crystallinity, glass transition temperature, polymer hydrophobicity, and molecular weight (MW), all of which relatively influence hydrolysis. Mathematical equations have been used to study the factors and mechanisms that affect drug dissolution compared to experimental release data. The equations used as models for predicting the kinetics of drug release include the zero-order, first-order, Higuchi, Hixson-Crowell, and Korsmeyer-Peppas equations. Aliphatic polyester-based controlled drug delivery has surrounded much of the current activity in the estimation parameters of nanoparticles and stimulated additional research. Polymeric nanoparticles have potential in a wide range of applications, such as in biotechnology, vaccine systems, and the pharmaceutical industry. The main goal of this chapter is to discuss aliphatic polyester nanoparticles as drug carrier systems.
15 August 2023 in Journal of Drug Delivery Science and Technology
Nicardipine hydrochloride‐loaded carboxymethyl cellulose/poly(D,L‐lactic‐co‐glycolic acid) nanocarriers were synthesized using a contemporary double emulsion process. The NCH‐CMC/PLGA nanocarriers can prolong the drug concentration and protect the drug from hydrolysis throughout a period of 16 days. The drug release kinetics indicated that the model followed the Korsmeyer‐peppas equation, leading to a combination of drug diffusion and polymer erosion. These nanocarriers could be an effective drug‐delivery agent for calcium channel blockers. More information can be found in the Full Paper by Narumol Kreua‐ongarjnukool, Sorayouth Chumnanvej et al.