Encapsulation of Nicardipine Hydrochloride and Release from Biodegradable Poly(D,L-lactic-co-glycolic acid) Microparticles by Double Emulsion Process: Effect of Emulsion Stability and Different Parameters on Drug Entrapment

Abstract

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 5.20 ± 0.25 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.

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

“…The swelling degree of the nanocarriers was determined by incubation at 37°C and pH 7.4 in phosphate-buffered saline (PBS) to simulate the body fluids in normal tissues. [15,18] The nanocarriers were synthesized according to the optimal parameters (see Section 1.5). The particle size of the nanocarriers was measured as~170 nm, and incubated samples were investigated using the DLS technique.…”

“…This phenomenon occurs because nanocarriers are less affected by the gravitational field than microparticles (5 μm), which will precipitate on the first day. [18] Polymeric nanocarriers with a zeta potential less than � 30 mV tend to aggregate faster. [35] The NCH-CMC/PLGA nanocarriers had a zeta potential of~20.4 mV, suggesting probable aggregation, with consistent zeta potential results after further PLGA addition (Figure 3).…”

“…To mimic the in vitro function of body fluids, drug release was evaluated by immersion in PBS (pH 7.4) at 37°C in a shaking bath with constant shaking at 70 rpm. [18] The release profile of nanocarriers included an initial burst release of NCH, as shown in Figure 11. After the burst, the nanocarriers were continuously released until a plateau was achieved at~70% release of the loaded drug after 16 days.…”

“…[15,17] Previously, PLGA carriers for NCH encapsulation have been via a double emulsion process. [13,18] The results showed that PLGA microparticles appeared to prevent NCH deterioration by hydrolysis. PLGA particles demonstrated a controlled release of the drug for 33 days and maintained a sufficient drug concentration.…”

“…In this study, carriers were synthesized with different ingredients using a contemporary emulsion process reported previously. [18] The nanocarriers with a distinctive architecture were obtained by adding CMC to the core of the carriers and a PLGA coating on the core. It was synthesized by a contemporary water in oil in water (W 1 /O/ W 2 ) double emulsion process.…”