scholarly journals IN VITRO AND IN VIVO EVALUATION OF FLOATING GASTRORETENTIVE DRUG DELIVERY SYSTEM OF CIMETIDINE USING HARD ALGINATE CAPSULES

2018 ◽  
Vol 11 (6) ◽  
pp. 162
Author(s):  
Ririyen Dessy N Siahaan ◽  
Hakim Bangun ◽  
Sumaiyah Sumaiyah
Keyword(s):  
Drug Delivery ◽  
Gastric Mucosa ◽  
Drug Release ◽  
Sustained Release ◽  
Drug Delivery System ◽  
Delivery System ◽  
Release Profile ◽  
Alginate Capsules

Objective: The objective of this study was to evaluate in vitro and in vivo of gastroretentive drug delivery system of cimetidine using hard alginate capsules.Methods: Drug release study was tested to various hard alginate capsules containing 200 mg cimetidine with paddle method dissolution apparatus in artificial gastric fluid pH 1.2. Concentrations of cimetidine were measured using ultraviolet spectrophotometer at 218.4 nm wavelength. The product that fulfilled the sustained release profile was evaluated for bioavailability using male rabbits at dose 9.3 mg/kg orally, and the antiulcer studies were evaluated by HCl-induced ulcer method at cimetidine dose 18 mg/kg once a day orally. Gastric lesions were evaluated by macroscopic and microscopic observations.Results: The results of drug release test showed that hard alginate capsule made from sodium alginate 500–600 cP gave sustained release profile of cimetidine for 12 h. In vivo bioavailability studies showed that cimetidine given with hard alginate capsules gave higher of Cmax, Tmax, and area under the curve of cimetidine compared to cimetidine that given with conventional hard gelatin capsules. The antiulcer studies showed that the healing effect of cimetidine that given with hard alginate capsules was faster than cimetidine given in suspension form. Cimetidine that given with hard alginate capsules macroscopically showed no gastric lesion and histopathologically also showed normal gastric mucosa of rats after 4 days treatment. However, cimetidine given in suspension form showed of 0.036±0.024 ulcer index and microscopically there was still erosion of gastric mucosa of rats after 4 days treatment.Conclusion: Floating gastroretentive of cimetidine using hard alginate capsules give a sustained release of cimetidine with better bioavailability and antiulcer effect of cimetidine.

In Vitro and In Vivo Drug Release from a Novel In Situ Forming Drug Delivery System

2007 ◽  
Vol 25 (6) ◽  
pp. 1347-1354 ◽  
Author(s):  
Heiko Kranz ◽  
Erol Yilmaz ◽  
Gayle A. Brazeau ◽  
Roland Bodmeier
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Drug Delivery System ◽  
Delivery System ◽  
In Situ Forming

A Smart Drug Delivery System Based on Thermo-Responsive Polymer Gated Au NRs@SiO2 Nano-Platform

2021 ◽  
Vol 16 (7) ◽  
pp. 1029-1036
Author(s):  
Hongzhu Wang ◽  
Mengxun Chen ◽  
Liping Song ◽  
Youju Huang
Keyword(s):  
Drug Delivery ◽  
Block Copolymer ◽  
Drug Release ◽  
Drug Delivery System ◽  
Delivery System ◽  
Photothermal Therapy ◽  
Drug Loading ◽  
Temperature Sensitive

A key challenge for nanoparticles-based drug delivery system is to achieve manageable drug release in tumour cell. In this study, a versatile system combining photothermal therapy and controllable drug release for tumour cells using temperature-sensitive block copolymer coupled Au NRs@SiO2 is reported. While the Au NRs serve as hyperthermal agent and the mesoporous silica was used to improve the drug loading and decrease biotoxicity. The block copolymer acted as “gatekeeper” to regulate the release of model drug (Doxorubicin hydrochloride, DOX). Through in vivo and in vitro experiments, we achieved the truly controllable drug release and photothermal therapy with the collaborative effect of the three constituents of the nanocomposites. The reported nanocomposites pave the way to high-performance controllable drug release and photothermal therapy system.

Floating Microsphere of Curcumin as Targeted Gastro-retentive Drug Delivery System

2021 ◽  
pp. 5202-5206
Author(s):  
Anupam K Sachan ◽  
Saurabh Singh ◽  
Kiran Kumari ◽  
Pratibha Devi
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Sustained Release ◽  
Drug Delivery System ◽  
Delivery System ◽  
Entrapment Efficiency ◽  
Synthetic Polymers ◽  
Drug Bioavailability ◽  
Gastric Residence Time

Microspheres carrier system made from natural or synthetic polymers used in sustained release drug delivery system. The present study involves formulation and evaluation of floating microspheres of Curcumin for improving the drug bioavailability by prolongation gastric residence time. Curcumin, natural hypoglycemic agent is a lipophilic drug, absorbed poorly from the stomach, quickly eliminated and having short half-life so suitable to formulate floating drug delivery system for sustained release. Floating microspheres of curcumin were formulated by solvent evaporation technique using ethanol and dichloromethane (1:1) as organic solvent and incorporating various synthetic polymers as coating polymer, sustain release polymers and floating agent. The final formulation were evaluated various parameters such as compatibility studies, micrometric properties, In-vitro drug release and % buoyancy. FTIR studies showed that there were no interaction between drug and excipients. The surface morphology studies by SEM confirmed their spherical and smooth surface. The mean particles size were found to be 416-618µm, practical yield of microspheres was in the range of 60.21±0.052% - 80.87±0.043%, drug entrapment efficiency 47.4±0.065% - 77.9±0.036% and % buoyancy 62,24±0.161% - 88.63±0.413%. Result show that entraptmency increased as polymer (Eudragit RS100) conc. Increased. The drug release after 12 hrs. was 72.13% - 87.13% and it decrease as a polymer (HPMC, EC) concentration was decrease.

scholarly journals Laser-activated drug implant for controlled release to the posterior segment of the eye

2020 ◽  
Author(s):  
Xingyu He ◽  
Zheng Yuan ◽  
Samantha Gaeke ◽  
Winston W.-Y. Kao ◽  
S. Kevin Li ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Drug Delivery System ◽  
Delivery System ◽  
Posterior Segment ◽  
Zero Order ◽  
First Order ◽  
Drug Implants

AbstractThe current standard of care for posterior segment eye diseases, such as age-related macular degeneration and diabetic macular edema, is frequent intravitreal injections or sustained-release drug implants. Drug implants have side effects due to the burst release of the drugs, and their release cannot be easily controlled after implantation. Present study attempts to develop a dosage-controllable drug delivery implant which consists of a nanoporous biodegradable PLGA capsule and light-activated liposomes. Controllable drug release from the implant was achieved by using pulsed near-infrared (NIR) laser both in vitro and in vivo. The in vitro drug release kinetics from two different initial dose implants, 1000 μg and 500 μg, was analyzed by fitting zero order and first order kinetics, as well as the Korsmeyer-Peppas and Higuchi models. The 1000 μg and 500 μg implants fit the first-order and zero-order kinetics model, respectively, the best. The multiple drug releases in the vitreous was determined by in vivo fluorimeter, which was consistent with the in vitro data. The dose released was also clinically relevant. Histology and optical and ultrasound imaging data showed no abnormality in the eyes received implant treatment suggesting that the drug delivery system was safe to the retina. This on-demand dose-controllable drug delivery system could be potentially used for long-term posterior eye disease treatment.

Design and preparation acid-activated montmorillonite sustained-release drug delivery system for dexibuprofen in vitro and in vivo evaluations

2018 ◽  
Vol 163 ◽  
pp. 178-185 ◽  
Author(s):  
Tingting Li ◽  
Lele Zhao ◽  
Ziliang Zheng ◽  
Min Zhang ◽  
Yidan Sun ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Sustained Release ◽  
Drug Delivery System ◽  
Delivery System ◽  
Release Drug

scholarly journals Eudraginated polymer blends: A potential oral controlled drug delivery system for theophylline

2012 ◽  
Vol 62 (1) ◽  
pp. 71-82 ◽  
Author(s):  
Martins Emeje ◽  
Lucy John-Africa ◽  
Yetunde Isimi ◽  
Olobayo Kunle ◽  
Sabinus Ofoefule
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Sustained Release ◽  
Polymer Blends ◽  
Drug Delivery System ◽  
Delivery System ◽  
Controlled Drug Delivery ◽  
Dosage Forms ◽  
Controlled Drug Delivery System

Eudraginated polymer blends: A potential oral controlled drug delivery system for theophylline Sustained release (SR) dosage forms enable prolonged and continuous deposition of the drug in the gastrointestinal (GI) tract and improve the bioavailability of medications characterized by a narrow absorption window. In this study, a new strategy is proposed for the development of SR dosage forms for theophylline (TPH). Design of the delivery system was based on a sustained release formulation, with a modified coating technique and swelling features aimed to extend the release time of the drug. Different polymers, such as Carbopol 71G (CP), sodium carboxymethylcellulose (SCMC), ethylcellulose (EC) and their combinations were tried. Prepared matrix tablets were coated with a 5 % (m/m) dispersion of Eudragit (EUD) in order to get the desired sustained release profile over a period of 24 h. Various formulations were evaluated for micromeritic properties, drug concentration and in vitro drug release. It was found that the in vitro drug release rate decreased with increasing the amount of polymer. Coating with EUD resulted in a significant lag phase in the first two hours of dissolution in the acidic pH of simulated gastric fluid (SGF) due to decreased water uptake, and hence decreased driving force for drug release. Release became faster in the alkaline pH of simulated intestinal fluid (SIF) owing to increased solubility of both the coating and matrixing agents. The optimized formulation was subjected to in vivo studies in rabbits and the pharmacokinetic parameters of developed formulations were compared with the commercial (Asmanyl®) formulation. Asmanyl® tablets showed faster absorption (tmax 4.0 h) compared to the TPH formulation showing a tmax value of 8.0 h. The Cmax and AUC values of TPH formulation were significantly (p < 0.05) higher than those for Asmanyl®, revealing relative bioavailability of about 136.93 %. Our study demonstrated the potential usefulness of eudraginated polymers for the oral delivery of the sparingly soluble drug theophylline.

Development of sustained release gastroretentive drug delivery system for ofloxacin: In vitro and in vivo evaluation

2005 ◽  
Vol 304 (1-2) ◽  
pp. 178-184 ◽  
Author(s):  
Mahesh Chavanpatil ◽  
Paras Jain ◽  
Sachin Chaudhari ◽  
Rajesh Shear ◽  
Pradeep Vavia
Keyword(s):  
Drug Delivery ◽  
Sustained Release ◽  
Drug Delivery System ◽  
Delivery System ◽  
In Vivo Evaluation

scholarly journals Design of DOX-GNRs-PNIPAM@PEG-PLA Micelle With Temperature and Light Dual-Function for Potent Melanoma Therapy

2021 ◽  
Vol 8 ◽  
Author(s):  
Na Wang ◽  
Jing Shi ◽  
Cong Wu ◽  
Weiwei Chu ◽  
Wanru Tao ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Drug Delivery System ◽  
Delivery System ◽  
Gold Nanorods ◽  
Dual Function ◽  
Serum Stability ◽  
Melanoma Therapy

Objective: The aim of this study was to construct light and temperature dual-sensitive micellar carriers loaded with doxorubicin (DOX) and gold nanorods (DOX-GNRs-PNIPAM@PEG-PLA, DAPP) for melanoma therapy.Methods: The DAPP self-assembled using fine-tuned physicochemical properties in water. The DAPP structure, temperature- and photo-sensitivity, drug-release, in-vitro serum stability, and cytotoxicity against melanoma B16F10 cells were evaluated in detail. The corresponding in-vitro and in-vivo therapeutic mechanisms were then evaluated using a B16F10-melanoma bearing BALB/c nude mouse model (B16F10).Results: The light and temperature sensitive micellar drug-delivery system assembled from block copolymer and gold nanorods exhibited a narrow particle size and size distribution, good biocompatibility, well-designed photo-temperature conversion, controlled drug release, and high serum stability. Compared with the free DOX- and PBS-treated groups, the cell endocytosis-mediated cytotoxicity and intra-tumor accumulation of DAPP was markedly enhanced by the NIR-light exposure and induced potent in-vivo tumor inhibitory activity.Conclusion: The design of DAPP, a dual-functional micellar drug-delivery system with temperature- and light-sensitive properties, offers a new strategy for skin-cancer therapy with a potent therapeutic index.

scholarly journals FORMULATION AND EVALUATION OF PULSATILE DRUG DELIVERY SYSTEM OF SALBUTAMOL SULFATE FOR THE CHRONOTHERAPY OF ASTHMA

2018 ◽  
Vol 11 (9) ◽  
pp. 305
Author(s):  
Chiranjibi Adhikari ◽  
Gururaj S Kulkarni ◽  
Shivakumar Swamy
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Drug Delivery System ◽  
Delivery System ◽  
Lag Time ◽  
Release Profile ◽  
Salbutamol Sulfate ◽  
Pulsatile Drug Delivery ◽  
Core Tablet

Objective: The main objective of the present study was to design and evaluate a time-controlled single unit oral pulsatile drug delivery system containing salbutamol sulfate for the prevention of nocturnal asthma attacks.Methods: Drug containing core tablets (C1-C10) with different composition of superdisintegrants such as sodium starch glycolate, croscarmellose sodium, and crospovidone were prepared by direct compression technique. The fast disintegrating core tablet formulation was selected, and press-coated tablets (P1-P11) were prepared with different compositions of hydrophobic and hydrophilic polymers: Ethylcellulose-20 (EC-20), hydroxypropyl methylcellulose K4M, and low substituted hydroxypropyl cellulose (L-HPC LH11). The coating polymers were selected and quantified based on in vitro lag time and drug release profile in simulated gastric and intestinal fluids.Results: Formulation C10 with 7.5% crospovidone showed least disintegrating time, i.e., 0.31 min and was selected as the best immediate release core tablet. The press-coated tablet formulation P11 having 360 mg barrier layer of EC-20 and L-HPC LH11 in ratio 14:1 over the core tablet C10 showed rapid and complete drug release nearly after 6 h lag time. Accelerated stability studies of the optimized formulation P11 indicated no significant difference in release profile after a period of 6 months.Conclusion: The in vitro dissolution study showed that lag time before drug release was highly affected by the coating level and nature of coating polymer used. Time-controlled pulsatile release tablets can be prepared using press-coating techniques.

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