Development of photostable gastro retentive formulation for nifedipine using low-density polypropylene microporous particles

Abstract

The aim of this study was to develop photostable gastro retentive formulation for nifedipine loading into low-density polypropylene microporous particles (Accurel MP 1000®) by a solvent evaporation technique using the 3² factorial design. Yield, drug loading, surface topography, thermal properties, crystal characteristics, photostability and in vitro drug release were studied. Optimized microparticles formulated into a capsule were evaluated for the dissolution study and compared with marketed formulation. Higher values of T(₅₀%), time required for 50% degradation of drug with threefold and 1.5-fold decrease in degradation rate constant (K) under UV and fluorescent lamp were observed for the microparticles, respectively, as compared to pure nifedipine indicated remarkable improved photostability. Microparticles showed good floating ability in 0.1N HCl with initial burst release (16-29%) followed by the zero-order drug release up to 8 h. The capsule formulation followed the ideal modified release pattern.

Investigation of Ethyl Cellulose Microsponge Gel for Topical Delivery of Eberconazole Nitrate for Fungal Therapy

“…The EBMG exhibited a burst effect within 2 h (98.3 ± 7.0 μg/cm 2 ) due to the presence of nonencapsulated drug closer to the surface or on the surface of the microsponges, which does not produce irritation to the skin. After that, a linear relationship existed for up to 12 h due to the porous nature of the microsponges providing the channel for drug release [22]. The slopes (flux) of the linear portion of the permeation profiles were calculated.…”

Production of functional spherical particles with porous hollow structures in water via oiling-out directional agglomeration

“…Nifedipine is extremely unstable to light and undergoes photocatalytic disproportionation of the molecule when exposed to light (i.e., degradation), producing nitro-pyridine derivatives and benzopyridine nitrite derivatives that are harmful to humans, which leads to harsh storage conditions for nifedipine. 67 As shown in Fig. 7a, nifedipine transforms from a brighter yellow-green color to a darker brownish-red color under sunlight exposure.…”

Developing Docetaxel-Loaded Nanocapsules: A Promising Approach for Cancer Therapy

“…To our knowledge, only a few examples in the literature deal with describing the effect of the drug state on its release kinetic from nanocarriers. Indeed, a significant change in the crystallinity of the polymer and the native drug may affect the drug release rate and subsequently its release kinetics [27] . Powdered X-ray Diffraction (PXRD) analysis revealed that DOC became amorphous and was likely to be dissolved within the NCs' oily core and probably in the PLA shell.…”