Monodispersed microparticles with a poly(D,L-lactide-co-glycolide) (PLGA) core and a poly(ethyl 2-cyanoacrylate) (PE2CA) shell were prepared by Shirasu porous glass (SPG) membrane emulsification to reduce the initial burst release of doxorubicin (DOX). Solution mixtures with different weight ratios of PLGA polymer and E2CA monomer were permeated under pressure through an SPG membrane with 1.9 µm pore size into a continuous water phase with sodium lauryl sulfate as a surfactant. Core-shell structured microparticles were formed by the mechanism of anionic interfacial polymerization of E2CA and precipitation of both polymers. The average diameter of the resulting microparticles with various PLGA:E2CA ratios ranged from 1.42 to 2.73 µm. The morphology and core-shell structure of the microparticles were observed by scanning electron microscopy (SEM) and transmission electron microscopy (TEM). The DOX release profiles revealed that the microparticles with an equivalent PLGA:E2CA weight ratio of 1:1 exhibited the optimal condition to reduce the initial burst of DOX. The initial release rate of DOX was dependent on the PLGA:E2CA ratio, and was minimized at a 1:1 ratio.
This article describes the topical delivery and localization of budesonide through the hairless mouse skin. Two poly(ethylene oxide)-block-poly(ε-caprolactone)-block-poly(ethylene oxide) (PEO-PCL-PEO) triblock copolymers (T 222 and T 252) having different CL:EO ratios were added in the preparation of budesonide particles stabilized with poly(vinyl alcohol) (PVA) and Tween 80 under ultrasonication. For comparison, a commercial PEO-PPO-PEO triblock copolymer (F68) was studied under the same condition. To demonstrate the effects of the triblock copolymer, the particle size of budesonide emulsion, entrapment efficiency, and in vitro release were measured and compared. The budesonide particles stabilized by the triblock copolymers had a diameter of ca. 350 nm with entrapment efficiencies of 66-76%. The In vitro release profiles of all samples showed an initial burst followed by sustained release. The skin penetration and permeation of budesonide were analyzed by using a Frantz diffusion cell. T 222 and T 252 exhibited higher total permeation amounts, but lower budesonide penetration amounts, than F68. The results suggest that the partitioning of budesonide in each skin layer can be adjusted in order to avoid skin thinning and negative immune response arising from the penetration of budesonide in blood vessels.
The objective of this study was to develop oral matrix tablets for the sustained release of vitamin C. In this study hydroxypropyl methylcellulose (HPMC) has been utilized as an excipient, as it is one of the most widely used polymers, for use during long periods of time in formations. The vitamin C tablet formulation depends on the molecular weight and concentration of sustained-delivery in HPMC. Anti-oxidants have been added as a dissolution medium in order to prevent vitamin C degradation in water. The dissolution test was carried out in a distilled water medium, and the release model equation was applied to analyze the vitamin C release pattern. The results demonstrated that the release and lasting power of vitamin C tablets, containing HPMC, lasted for more than 12 h.
This article describes the preparation and characterization of hydroxypropyl methylcellulose-graftpoly(ethylacrylate-co-methyl methacrylate) particles [HPMC-g-poly(EA-co-MMA) NPs]. The particles were prepared by resin-fortified emulsion polymerization using ceric ammonium nitrate (CAN). In this study, a series of HPMC-g-poly(EA-co-MMA) NPs were synthesized by varying the CAN : HPMC and HPMC : (EA/MMA) ratios to determine the effects of these variables on the physical properties of HPMC-g-poly(EA-co-MMA) as well as the dissolution behavior of an aspirin tablet, as a model drug. The drug dissolution profiles of the coated tablets were affected significantly by the HPMC : (EA/MMA) molar ratio.
This article presents an evaluation of the effects of coating conditions on the enteric coating quality of soft gelatin capsules containing Omega-3 fatty acids. Three conditions were controlled: concentration of hydroxypropyl methylcellulose phthalate (6, 8, and 10 wt% in solution), temperature of the inlet air (32, 35, and 38 o C), and the coating solution feed rate (7.5, 11.25, and 15.0 g/min). The transparency of the enteric coated soft gelatin capsules was evaluated by measuring the degree of whiteness of the surface using a spectrophotometer. Results showed that the most important parameter in the enteric coating process was the coating solution feed rate. As the coating solution feed rate decreased and inlet air temperature increased, the degree of whiteness of coating surfaces decreased. We also evaluated the disintegration properties of the enteric coated capsules in accordance with the Korea Health Functional Food Code.
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