Search results for "RELEASE"
showing 10 items of 602 documents
Loading, release and stability of epirubicin-loaded drug-eluting beads.
2015
Purpose The aim of this study was to determine the loading efficiency, physico-chemical stability and release of epirubicin-loaded DC Bead™ (Biocompatibles UK Ltd, a BTG International group company) (bead size 70–150 µm (=DC Bead M1™) and 100–300 µm) after loading with epirubicin solution (2 mg/ml) or reconstituted powder formulation (25 mg/ml) and controlled storage. Methods DC Bead™ were loaded with 76 mg epirubicin solution (Epimedac™, Medac GmbH) or 75 mg epirubicin powder formulation (Farmorubicin™, Pharmacia Pfizer GmbH) per 2 ml of beads. Drug loading efficiency and stability were determined by measuring the epirubicin concentration in the excess solution after predetermined interval…
Tailoring the physicochemical properties of core-crosslinked polymeric micelles for pharmaceutical applications.
2016
To optimally exploit the potential of (tumor-) targeted nanomedicines, platform technologies are needed in which physicochemical and pharmaceutical properties can be tailored according to specific medical needs and applications. We here systematically customized the properties of core-crosslinked polymeric micelles (CCPM). The micelles were based on mPEG-b-pHPMAmLacn (i.e. methoxy poly(ethylene glycol)-b-poly[N-(2-hydroxypropyl) methacrylamide-lactate]), similar to the block copolymer composition employed in CriPec® docetaxel, which is currently in phase I clinical trials. The CCPM platform was tailored with regard to size (30 to 100 nm), nanocarrier degradation (1 month to 1 year) and drug…
Modified Montmorillonite as Drug Delivery Agent for Enhancing Antibiotic Therapy
2021
The appealing properties of surfactant-intercalated Montmorillonites (Organo-montmorillonite, OMt) were successfully investigated to propose an effective drug delivery system for metronidazole (MNE) antibiotic therapy. This represents a serious pharmaceutical concern due to the adverse drug reactions and the low targeting ability of MNE. The non-ionic surfactant Tween 20 was used to functionalize montmorillonite, thus accomplishing the two-fold objective of enhancing the stability of clay dispersion and better controlling drug uptake and release. The adsorption process was performed under different experimental conditions and investigated by constructing the adsorption isotherms through hig…
Efficacy of budesonide-loaded mesoporous silica microparticles capped with a bulky azo derivative in rats with TNBS-induced colitis.
2019
Abstract A colon targeted drug delivery system for inflammatory bowel diseases (IBD), consisting in budesonide loaded mesoporous silica microparticles functionalized with a selective azo-molecular gate (M-Bud), has been evaluated for in vivo efficacy. Experimental colitis in male Wistar rats was induced by rectal instillation of 2,4,6-trinitrobenzenesulfonic acid (TNBS). M-Bud was orally administered to the rats as a suspension in water. Colon/body weight ratio, clinical activity score, and histological evaluation were used as inflammatory indices to measure the performance of the microparticles. The formulation was compared with a suspension prepared from the commercial drug Entocord®. Sta…
Entrapment of an EGFR inhibitor into nanostructured lipid carriers (NLC) improves its antitumor activity against human hepatocarcinoma cells
2014
Background: In hepatocellular carcinoma (HCC), different signaling pathways are de-regulated, and among them, the expression of the epidermal growth factor receptor (EGFR). Tyrphostin AG-1478 is a lipophilic low molecular weight inhibitor of EGFR, preferentially acting on liver tumor cells. In order to overcome its poor drug solubility and thus improving its anticancer activity, it was entrapped into nanostructured lipid carriers (NLC) by using safe ingredients for parenteral delivery. Results: Nanostructured lipid carriers (NLC) carrying tyrphostin AG-1478 were prepared by using the nanoprecipitation method and different matrix compositions. The best system in terms of mean size, PDI, zeta…
Montmorillonite nanodevices for the colon metronidazole delivery.
2013
The adsorption profiles of the antibiotic metronidazole (MNE) into the K10-montmorillonite (MMT-K10) clay and the subsequent release have been investigated as a function of pH and MNE/MMT-K10 ratio, in order to evaluate the potential of the MNE/MMT-K10 hybrids as controlled drug delivery system. The adsorption mechanism has been first elucidated by performing complementary equilibrium and kinetic studies and through the X-ray diffractometry (XRD) characterization of the obtained composite materials. The gathered results allowed us to propose a mechanism consisting of a multi-step pathway involving the neutral and the cationic form of the drug, which interact with different sites of the clay…
Biowaiver monographs for immediate release solid oral dosage forms: efavirenz.
2013
Literature data pertaining to the decision to allow a waiver of in vivo bioequiv- alence testing for the approval of immediate-release (IR) solid oral dosage forms containing efavirenz as the only active pharmaceutical ingredient (API) are reviewed. Because of lack of conclusive data about efavirenz's permeability and its failure to comply with the "high solu- bility" criteria according to the Biopharmaceutics Classification System (BCS), the API can be classified as BCS Class II/IV. In line with the solubility characteristics, the innovator product does not meet the dissolution criteria for a "rapidly dissolving product." Furthermore, product variations containing commonly used excipients …
PLGA nanoparticles are effective to control the colonic release and absorption on ibuprofen.
2018
The oral controlled release (CR) formulations have become more important in recent years. Among them, the polymeric nanoparticles have been thoroughly studied during the last decades, consequently they are extensively employed for a broad range of applications and drugs. The objective of this research was to develop polymeric nanoparticles (NPs) of ibuprofen with poly(lactic-co-glycolic) acid (PLGA) as polymer, and to test their applicability for oral CR formulations development. Different proportions of drug/polymer were employed to develop the ibuprofen NPs and their in vitro release profiles were analysed. The in situ segmental permeability of ibuprofen was tested in Wistar rat and demon…
In VitroRelease of Local Anaesthetic and Anti-Inflammatory Drugs from Crosslinked Collagen Based Device
2012
The drug delivery systems that are the object of this article take the form of a hydrophilic matrix (collagen or crosslinked collagen) containing a drug. These devices can be used as The model active agents, were chosen from the range of local anaesthetics (lidocaine hydrochloride), anti-inflammatory (diclofenac sodium salt) and antioxydant (caffeic acid). Whatever the drug affinity for water, in the first time of the experiments, the release appears to be systematically delayed when the matrix is crosslinked. For lidocaine hydrochloride based systems, as the amount of drug increases in the matrix, the high gap concentration between the matrix and the buffer solution promote the diffusion a…
Polymer-based systems for controlled release and targeting of drugs
2019
The current need to find new advanced approaches to carry biologically active substances (conventional organic drugs, peptides, proteins (such as antibodies), and nucleic acid-based drugs (NABDs such as siRNA and miRNA)) in the body fluids, to realize targeted therapies and even personalized ones, goes hand in hand with research on the performance of new materials to better realize appropriate drug vectors [...]