Indomethacin uptake into poly(2-hydroxyethyl methacrylate-co-3,9-divinyl-2,4,8,10-tetraoxaspiro [5.5]-undecane) network: In vitro and in vivo controlled release study

2012 ◽  
Vol 426 (1-2) ◽  
pp. 90-99 ◽  
Author(s):  
Loredana E. Nita ◽  
Aurica P. Chiriac ◽  
Manuela T. Nistor ◽  
Liliana Tartau
Keyword(s):  
Controlled Release ◽  
Hydroxyethyl Methacrylate ◽  
Release Study

scholarly journals In vitro kinetic release study, antimicrobial activity and in vivo toxicity profile of a kojic acid ester-based nanoemulsion for topical application

RSC Advances ◽  
2020 ◽  
Vol 10 (71) ◽  
pp. 43894-43903
Author(s):  
Sharifah Nurfadhlin Afifah Syed Azhar ◽  
Siti Efliza Ashari ◽  
Syahida Ahmad ◽  
Norazlinaliza Salim
Keyword(s):  
Drug Delivery ◽  
Antimicrobial Activity ◽  
Controlled Release ◽  
Topical Application ◽  
Kojic Acid ◽  
Toxicity Profile ◽  
Kinetic Release ◽  
Release Study

Nanoemulsions have emerged as novel vehicles for drug delivery that allow sustained or controlled release for topical application.

Development, in vitro and in vivo Evaluations of Solid-Lipid Microparticles based on Solidified Micellar Carrier System for Oral Delivery of Cefepime

2017 ◽  
Vol 10 (1) ◽  
pp. 3582-3593
Author(s):  
Chukwuebuka Umeyor ◽  
Uchechukwu Nnadozie ◽  
Anthony Attama
Keyword(s):  
Oral Delivery ◽  
In Vitro Release ◽  
Carrier System ◽  
Solid Lipid ◽  
Solid Lipid Microparticles ◽  
Release Study ◽  
Lipid Microparticles ◽  
Vitro Release

This study seeks to formulate and evaluate a solid lipid nanoparticle-based, solidified micellar carrier system for oral delivery of cefepime. Cefepime has enjoyed a lot of therapeutic usage in the treatment of susceptible bacterial infections; however, its use is limited due to its administration as an injection only with poor patient compliance. Since oral drug administration encourage high patient compliance with resultant effect in improved therapy, cefepime was formulated as solid lipid microparticles for oral delivery using the concept of solidified micellar carrier system. The carrier system was evaluated based on particle yield, particle size and morphology, encapsulation efficiency (EE %), and thermal analysis using differential scanning calorimeter (DSC). Preliminary microbiological studies were done using gram positive and negative bacteria. In vitro release study was performed using biorelevant media, while in vivo release study was performed in white albino rats. The yield of solid lipid microparticles (SLM) ranged from 84.2 – 98.0 %. The SLM were spherical with size ranges of 3.8 ± 1.2 to 42.0 ± 1.4 µm. The EE % calculated ranged from 83.6 – 94.8 %. Thermal analysis showed that SLM was less crystalline with high potential for drug entrapment. Microbial studies showed that cefepime retained its broad spectrum anti-bacterial activity. In vitro release showed sustained release of cefepime from SLM, and in vivo release study showed high concentration of cefepime released in the plasma of study rats. The study showed that smart engineering of solidified micellar carrier system could be used to improve oral delivery of cefepime.

scholarly journals Predicting absorption and pharmacokinetic profile of carbamazepine from controlled-release tablet formulation in humans using rabbit model

2011 ◽  
Vol 65 (1-2) ◽  
pp. 71-81
Author(s):  
Irena Homsek ◽  
Dragica Popadic ◽  
Slobodanka Simic ◽  
Slavica Ristic ◽  
Katarina Vucicevic ◽  
...  
Keyword(s):  
Controlled Release ◽  
Rabbit Model ◽  
Tablet Formulation ◽  
Human Model ◽  
In Vitro Dissolution ◽  
Pharmacokinetic Parameters ◽  
Pharmacokinetic Data ◽  
Drug Concentrations

Controlled-release (CR) pharmaceutical formulations offer several advantages over the conventional, immediate release dosage forms of the same drug, including reduced dosing frequency, decreased incidence and/or intensity of adverse effects, greater selectivity of pharmacological activity, reduced drug plasma fluctuation, and better compliance. After a drug product has been registered, and is already on market, minor changes in formulation might be needed. At the same time, the product has to remain effective and safe for patients that could be confirmed via plasma drug concentrations and pharmacokinetic characteristics. It is challenging to predict human absorption and pharmacokinetic characteristics of a drug based on the in vitro dissolution test and the animal pharmacokinetic data. Therefore, the objective of this study was to establish correlation of the pharmacokinetic parameters of carbamazepine (CBZ) CR tablet formulation between the rabbit and the human model, and to establish in vitro in vivo correlation (IVIVC) based on the predicted fractions of absorbed CBZ. Although differences in mean plasma concentration profiles were notified, the data concerning the predicted fraction of drug absorbed were almost superimposable. Accordingly, it can be concluded that rabbits may be representative as an in vivo model for predicting the pharmacokinetics of the CR formulation of CBZ in humans.

scholarly journals ANTIULCER ACTIVITY OF CONTROLLED RELEASE FORMULATION CONTAINING AQUEOUS EXTRACT OF ACACIA CATECHU WILLD ON RODENT MODELS

2018 ◽  
Vol 10 (5) ◽  
pp. 25
Author(s):  
Basant Khare ◽  
Naina Dubey ◽  
Akash Sharma
Keyword(s):  
Controlled Release ◽  
Aqueous Extract ◽  
Maximum Activity ◽  
Antiulcer Activity ◽  
Rodent Models ◽  
Ulcer Index ◽  
Release Formulation ◽  
Acacia Catechu

Objective: To study the Antiulcer activity of aqueous extract of acacia catechu willd on rodent models by controlled release formulation.Methods: Microspheres were prepared by solvent evapoaration method and were evaluated for various parameters like SEM, stability and in vitro relese. And acacia catechu willd loaded microspheres were evaluated for in vivo study involving Gastric ulceration in rats was induced by Ethanol/HCl. Ulcer genic effect (Ulcer Index), pH and Total acidity, Histopathological studies.Results: Results indicated that Acacia catechu willd microspheres contains some active constituents like flavanoid which are responsible for its anti ulcer activity. Also it was observed aqueous extract loaded microspheres showed maximum activity was found (200 mg/kg) with standard Cimetidine (100 mg/kg) also, the results revealed that aqueous extract microspheres at 200 mg/kg had reduced ulcer incidence significantly, when compared to the control as evident by decrease in ulcer score in the model.Conclusion: Based on the result it can be concluded that microspheres loaded with aqueous extracts of Acacia catechu willd produced promising antiulcer activity and were safe.

scholarly journals FORMULATION, OPTIMIZATION, CHARACTERIZATION AND IN VIVO ANTI-ULCER ACTIVITY OF ESOMEPRAZOLE MAGNESIUM TRIHYDRATE GASTRORESISTANT MICROSPHERES

2016 ◽  
Vol 9 (1) ◽  
pp. 273
Author(s):  
Krutika Sawant ◽  
Mitali Patel ◽  
Jiten Patel ◽  
Piyush Mundada
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Intestinal Absorption ◽  
Ulcer Formation ◽  
Scanning Calorimetry ◽  
Aqueous Solvent ◽  
Release Study ◽  
Esomeprazole Magnesium

<p><strong>Objective: </strong>The objective of the present investigation was to prepare gastro-resistant microspheres of esomeprazole magnesium trihydrate (EMT) to prevent its degradation in the acidic environment of the stomach and enhance its bioavailability via intestinal absorption.</p><p><strong>Methods: </strong>EMT loaded gastro-resistant microspheres were prepared using hypromellose acetate succinate (HPMCAS) as the gastro-resistant polymer by ‘non-aqueous solvent evaporation’ technique. A 3-factor 3 level factorial design was used to optimise EMT: HPMCAS ratio, the concentration of Span 80 and stirring speed with respect to percent entrapment efficiency and particle size. Further characterization was carried out using scanning electron microscopy (SEM), differential scanning calorimetry (DSC), <em>In vitro</em> release study and <em>In vivo</em> anti-ulcer activity.</p><p><strong>Results: </strong>Fourier transform infrared <strong>(</strong>FTIR) study indicated compatibility between drug and polymer. DSC study revealed that the drug was molecularly dispersed in the polymer. The optimised batch showed 49.63±1.23% drug entrapment and 170.12±3.36 μm particle size. SEM study showed that microspheres were spherical in shape<strong>. </strong><em>In vitro</em> drug release study showed only 4.28±1.23% drug release in simulated gastric media in 2 hr and 93.46±1.20% release in simulated intestinal media after 1 hr from the optimised batch.</p><p><strong>Conclusion: </strong>Results of <em>in vitro </em>release studies indicated the gastro-resistant nature of the developed microspheres. <em>In vivo</em> anti-ulcer activity demonstrated that EMT loaded microspheres were able to significantly reduce ethanol-induced ulcer formation in rats’ stomach as compared to the aqueous solution of EMT. So it can be concluded that the developed gastro-resistant microspheres of EMT prevented drug release in the stomach which would lead to a significant improvement in its bioavailability through enhanced intestinal absorption</p>

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