Nanoemulsion Loaded with Clotrimazole Based on Rapeseed Oil for Potential Vaginal Application-Development, Initial Assessment, and Pilot Release Studies.

Vaginal candidiasis (VC) is an emerging global hardly treated health issue affecting millions of women worldwide. In this study, the nanoemulsion consisting of clotrimazole (CLT), rapeseed oil, Pluronic F-68, Span 80, PEG 200, and lactic acid was prepared using high-speed and high-pressure homogenization. Yielded formulations were characterized by an average droplet size of 52-56 nm, homogenous size distribution by volume, and a polydispersity index (PDI) < 0.

Towards a Better Understanding of Verapamil Release from Kollicoat SR:IR Coated Pellets Using Non-Invasive Analytical Tools.

The aim of this study was to gain deeper insight into the mass transport mechanisms controlling drug release from polymer-coated pellets using non-invasive analytical tools. Pellet starter cores loaded with verapamil HCl (10% loading, 45% lactose, 45% microcrystalline cellulose) were prepared by extrusion/spheronization and coated with 5% Kollicoat SR:IR 95:5 or 10% Kollicoat SR:IR 90:10. Drug release was measured from ensembles of pellets as well as from single pellets upon exposure to acetate buffer pH = 3.

Robustness of Controlled Release Tablets Based on a Cross-linked Pregelatinized Potato Starch Matrix.

The aim of this study was to evaluate the potential of a cross-linked pregelatinized potato starch (PREGEFLO® PI10) as matrix former for controlled release tablets. Different types of tablets loaded with diprophylline, diltiazem HCl or theophylline were prepared by direct compression of binary drug/polymer blends. The drug content was varied from 20 to 50%.

Formulation and Coating of Alginate and Alginate-Hydroxypropylcellulose Pellets Containing Ranolazine.

The formulation and the coating composition of biopolymeric pellets containing ranolazine were studied to improve their technological and biopharmaceutical properties. Eudragit L100 (EU L100) and Eudragit L30 D-55-coated alginate and alginate-hydroxypropylcellulose (HPC) pellets were prepared by ionotropic gelation using 3 concentrations of HPC (0.50%, 0.

Importance of air bubbles in the core of coated pellets: Synchrotron X-ray microtomography allows for new insights.

High-resolution X-ray microtomography was used to get deeper insight into the underlying mass transport mechanisms controlling drug release from coated pellets. Sugar starter cores were layered with propranolol HCl and subsequently coated with Kollicoat SR, plasticized with 10% TEC. Importantly, synchrotron X-ray computed microtomography (SR-μCT) allowed direct, non-invasive monitoring of crack formation in the film coatings upon exposure to the release medium.

Accelerated ketoprofen release from spray-dried polymeric particles: importance of phase transitions and excipient distribution.

HPMC-, PVPVA- and PVP-based microparticles loaded with 30% ketoprofen were prepared by spray drying suspensions or solutions in various water:ethanol blends. The inlet temperature, drying gas and feed flow rates were varied. The resulting differences in the ketoprofen release rates in 0.

Accelerated ketoprofen release from polymeric matrices: importance of the homogeneity/heterogeneity of excipient distribution.

Polymeric matrices loaded with 10-50% ketoprofen were prepared by hot-melt extrusion or spray-drying. Eudragit E, PVP, PVPVA and HPMC were studied as matrix formers. Binary "drug-Eudragit E" as well as ternary "drug-Eudragit E-PVP", "drug-Eudragit E-PVPVA" and "drug-Eudragit E-HPMC" combinations were investigated and characterized by optical macro/microscopy, SEM, particle size measurements, mDSC, X-ray diffraction and in vitro drug release studies in 0.

Mechanisms controlling theophylline release from ethanol-resistant coated pellets.

Purpose: To elucidate the mass transport mechanisms controlling drug release from recently proposed, ethanol-resistant, polymeric film coatings.

Methods: Theophylline matrix pellets were coated with ethylcellulose: guar gum blends. Drug release from single pellets and ensembles of pellets was measured in various release media.

Ethanol-resistant ethylcellulose/guar gum coatings--importance of formulation parameters.

Recently, ethylcellulose/guar gum blends have been reported to provide ethanol-resistant drug release kinetics from coated dosage forms. This is because the ethanol insoluble guar gum effectively avoids undesired ethylcellulose dissolution in ethanol-rich bulk fluids. However, so far the importance of crucial formulation parameters, including the minimum amount of guar gum to be incorporated and the minimum required guar gum viscosity, remains unclear.

Ethanol-resistant polymeric film coatings for controlled drug delivery.

The sensitivity of controlled release dosage forms to the presence of ethanol in the gastro intestinal tract is critical, if the incorporated drug is potent and exhibits severe side effects. This is for instance the case for most opioid drugs. The co-ingestion of alcoholic beverages can lead to dose dumping and potentially fatal consequences.

Drug release mechanisms from Kollicoat SR:Eudragit NE coated pellets.

Thin, free films based on Kollicoat SR:Eudragit NE blends were prepared by casting or spraying aqueous dispersions of these polymers, and were thoroughly characterized with respect to their water uptake behavior, water permeability, dry mass loss kinetics, mechanical properties and drug release patterns. A mechanistic mathematical model based on Fick's law of diffusion was used to quantify the experimentally measured release of metoprolol succinate from various types of systems. With increasing Eudragit NE content the films became more hydrophobic, resulting in decreased water permeability as well as water uptake rates and extents.

Dynamic and static curing of ethylcellulose:PVA-PEG graft copolymer film coatings.

When using aqueous polymer dispersions for the preparation of controlled-release film coatings, instability during long-term storage can be a crucial concern. Generally, a thermal after treatment is required to assure sufficient polymer particle coalescence. This curing step is often performed under static conditions in an oven, which is a time-consuming and rather cumbersome process.

Simulated food effects on drug release from ethylcellulose: PVA-PEG graft copolymer-coated pellets.

Background: Food effects might substantially alter drug release from oral controlled release dosage forms in vivo.

Methods: The robustness of a novel type of controlled release film coating was investigated using various types of release media and two types of release apparatii.

Results: Importantly, none of the investigated conditions had a noteworthy impact on the release of freely water-soluble diltiazem HCl or slightly water-soluble theophylline from pellets coated with ethylcellulose containing small amounts of PVA-PEG graft copolymer.

Effects of film coating thickness and drug layer uniformity on in vitro drug release from sustained-release coated pellets: a case study using terahertz pulsed imaging.

Film coating thickness and terahertz electric field peak strength (TEFPS) were determined using terahertz pulsed imaging (TPI) and employed for the analysis of sustained-release coated pellets (theophylline layered sugar cores coated with Kollicoat SR:Kollicoat IR polymer blends). The effects of coating thickness, drug layer uniformity and optional curing were investigated using eight batches of pellets. Ten pellets from each batch were imaged with TPI to analyse the coating morphology (depicted in TEFPS) and thickness prior to release measurements.

Drug release mechanisms from ethylcellulose: PVA-PEG graft copolymer-coated pellets.

The aim of this study was to better understand the underlying drug release mechanisms from aqueous ethylcellulose-coated pellets containing different types of drugs and starter cores. Theophylline, paracetamol, metoprolol succinate, diltiazem HCl and metoprolol tartrate were used as model drugs exhibiting significantly different solubilities (e.g.

Prediction of drug release from ethylcellulose coated pellets.

The aim of this study was to elucidate the underlying drug release mechanisms in pellets coated with aqueous ethylcellulose dispersion, providing long term stable drug release profiles and containing different types of starter cores. The systems were thoroughly characterized using mechanical analysis; the sensitivity of drug release to the osmolality of the release medium was measured; scanning electron microscopy and optical macroscopy were used to monitor the pellets' morphology and dimensions upon exposure to different media, and drug release was measured from single and ensembles of pellets as well as from thin, free films. All experimental results indicate that diltiazem HCl release from pellets coated with ethylcellulose containing small amounts of poly(vinyl alcohol)-poly(ethylene glycol) graft copolymer is primarily controlled by drug diffusion through the intact polymeric membranes, irrespective of the type of starter core (consisting of microcrystalline cellulose or sugar, optionally coated with ethylcellulose).

Improved long term stability of aqueous ethylcellulose film coatings: importance of the type of drug and starter core.

Instability during long term storage due to further gradual coalescence of the film remains one of the major challenges when using aqueous polymer dispersions for controlled release coatings. It has recently been shown that the addition of small amounts of poly(vinyl acetate)-poly(ethylene glycol)-graft-copolymer (PVA-PEG-graft-copolymer) to aqueous ethylcellulose dispersion provides long term stable drug release patterns even upon open storage under stress conditions in the case of theophylline matrix cores. However, the transferability of this approach to other types of drugs and starter cores exhibiting different osmotic activity is yet unknown.

How to improve the storage stability of aqueous polymeric film coatings.

The major aim of this study was to identify an easy tool to improve the long term stability of polymeric film coatings applied from aqueous dispersions. Drug release profiles from ethylcellulose-coated theophylline pellets were monitored during 6 months open storage under ambient and stress conditions ["room temperature/ambient relative humidity (RH)" and "40 degrees C/75%RH"]. The pellets were cured for 1 or 2 d at 60 degrees C or for 1 or 2 d at 60 degrees C/75%RH (followed by 1 d at 60 degrees C for drying).

Controlled drug release from Gelucire-based matrix pellets: experiment and theory.

The aim of this work was to elucidate the underlying drug release mechanisms from lipidic matrix pellets, using theophylline and Gelucire 50/02 as model drug and carrier material, respectively. Pellets were prepared by two different techniques: melt-solidification and extrusion-spheronization. The effects of different formulations and processing parameters on the resulting drug release kinetics in 0.