Cellulose Acetate Microspheres as Floating Depot Systems to Increase Gastric Retention of Antidiabetic Drug: Formulation, Characterization and In Vitro–In Vivo Evaluation

Choudhury, Pratim Kumar; Kar, Manoranjan; Chauhan, Chetan Singh

doi:10.1080/03639040701542531

Cited by 29 publications

(22 citation statements)

References 12 publications

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“…Preparation of microparticles using oil in oil (o/o) solvent evaporation technique resulted in a spherical microparticle with continuous coating and no aggregation (Shivhare et al, 2009). Choudhury et al (2008) prepared cellulose acetate microspheres for gastric retention by emulsion-solvent evaporation method. When different polymer:drug concentration ratios (2:1 and 4:1) were used for the preparation of microspheres, the mean particle sizes and buoyancy percentage were found to be 7 and 18 microns, and $56% and $88%, respectively.…”

Section: Metformin-loaded Microparticles and Nanoparticlesmentioning

confidence: 99%

Microparticulate and nanoparticulate drug delivery systems for metformin hydrochloride

Çetin

Şahin

2015

Drug Delivery

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Context: Metformin hydrochloride is a biguanide derivative widely used for the treatment of type 2 diabetes, prescribed nearly to 120 million people worldwide. Metformin has a relatively low oral bioavailability (about 50-60%). Although the major effect of metformin is to decrease hepatic glucose output as an antihyperglycemic agent, its inhibitory effects on the proliferation of some cancer cells (e.g. prostate, breast, glioma cells) have been demonstrated in the cell culture studies. Development of novel formulation (e.g. microparticles, nanoparticles) strategies for metformin might be useful to improve its bioavailability, to reduce the dosing frequency, to decrease gastrointestinal side effects and toxicity and to be helpful for effective use of metformin in cancer treatment. Objective: The main aim of this review is to summarize metformin HCl-loaded micro-and nanoparticulate drug delivery systems. Method: The literature was rewieved with regard to the physicochemical, pharmacological properties of metformin, and also its mechanism of action in type 2 diabetes and cancer. In addition, micro-and nanoparticulate drug delivery systems developed for metformin were gathered from the literature and the results were discussed. Conclusion: Metformin is an oral antihyperglycemic agent and also has potential antitumorigenic effects. The repeated applications of high doses of metformin (as immediate release formulations) are needed for an effective treatment due to its low oral bioavailability and short biological half-life. Drug delivery systems are very useful systems to overcome the difficulties associated with conventional dosage forms of metformin and also for its effective use in cancer treatment.

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Section: Metformin-loaded Microparticles and Nanoparticlesmentioning

confidence: 99%

Microparticulate and nanoparticulate drug delivery systems for metformin hydrochloride

Çetin

Şahin

2015

Drug Delivery

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“…Floating systems do not bind with mucosal surfaces in the body and reduce the safety problems associated with mucoadhesive systems (6). Multiparticulate systems avoid the "all or none" gastric emptying process of the single unit system (7,8). Keeping in view all these factors, amoxicillin-loaded GFS was designed and optimized to increase the residence time of the drug in the stomach without contact with the mucosa.…”

Section: Introductionmentioning

confidence: 99%

Optimization Studies on Gastroretentive Floating System Using Response Surface Methodology

Awasthi¹,

Kulkarni²,

Pawar³

et al. 2011

AAPS PharmSciTech

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Abstract. The aim of the present investigation was to develop and optimize gastroretentive floating system of amoxicillin for the efficient treatment of peptic ulcer induced by Helicobacter pylori infection. Floating microballoons were developed using central composite design (CCD), and optimization was done by employing response surface methodology. The selected independent variables were cellulose acetate phthalate, drug-Eudragit S100 ratio, and the ratio of dichloromethane/ethanol/isopropyl alcohol. The selected dependent variables were yield, mean particle size, buoyancy, encapsulation efficiency, and drug release within 8 h. A quadratic polynomial model was generated which had linear, interaction, and quadratic terms to predict and evaluate the independent variables with respect to the dependent variables. Results showed that selected independent variables significantly affect the yield (30.53-82.71%), particle size (31.62-47.03 μm), buoyancy (42.68-95.75%), encapsulation efficiency (56.96-93.13%), and cumulative drug release from the microballoons (34.01-74.65%). The interaction and quadratic terms were also found to affect the process variables. An excellent agreement was found between the actual value and predicted value. In conclusion, it can be said that CCD is a valuable second-degree design to develop and optimize GFS of amoxicillin which in turn provides a basis to localize the drug release in the gastric region for effective treatment of H. pylori-mediated infection.

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“…With increased polymer concentration, the viscosity of the medium increased, resulting in enhanced interfacial tension that led to a decrease in the shearing efficiency and resulted in formation of larger-sized microparticles (13). On the other hand, increasing concentration of surfactant lowered the interfacial tension, enhanced due to increase in polymer concentration and prevented droplet coalescence that led to reduction in size of microparticles (14). Thus for a given drug: polymer ratio, an increase in surfactant resulted in decrease in particle size for both set of formulations.…”

Section: Micromeritic Propertiesmentioning

confidence: 99%

Design and In Vitro Performance Evaluation of Purified Microparticles of Pravastatin Sodium for Intestinal Delivery

Garg

Pathak

2011

AAPS PharmSciTech

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Abstract. The purpose of research was to develop a mucoadhesive multiparticulate sustained drug delivery system of pravastatin sodium, a highly water-soluble and poorly bioavailable drug, unstable at gastric pH. Mucoadhesive microparticles were formulated using eudragit S100 and ethyl cellulose as mucoadhesive polymers. End-step modification of w/o/o double emulsion solvent diffusion method was attempted to improve the purity of the product, that can affect the dose calculations of sustained release formulations and hence bioavailability. Microparticles formed were discrete, free flowing, and exhibited good mucoadhesive properties. DSC and DRS showed stable character of drug in microparticles and absence of drug polymer interaction. The drug to polymer ratio and surfactant concentration had significant effect on mean particle size, drug release, and entrapment efficiency. Microparticles made with drug: eudragit S100 ratio of 1:3 (F6) exhibited maximum entrapment efficiency of 72.7% and ex vivo mucoadhesion time of 4.15 h. In vitro permeation studies on goat intestinal mucosa demonstrated a flux rate (1,243 μg/cm 2 /h) that was 169 times higher than the flux of pure drug. The gastric instability problem was overcome by formulating the optimized microparticles as enteric-coated capsules that provided a sustained delivery of the highly water-soluble drug for 12 h beyond the gastric region. The release mechanism was identified as fickian diffusion (n=0.4137) for the optimized formulation F6. Conclusively, a drug delivery system was successfully developed that showed delayed and sustained release up to 12 h and could be potentially useful to overcome poor bioavailability problems associated with pravastatin sodium.

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Cellulose Acetate Microspheres as Floating Depot Systems to Increase Gastric Retention of Antidiabetic Drug: Formulation, Characterization and In Vitro–In Vivo Evaluation

Cited by 29 publications

References 12 publications

Microparticulate and nanoparticulate drug delivery systems for metformin hydrochloride

Microparticulate and nanoparticulate drug delivery systems for metformin hydrochloride

Optimization Studies on Gastroretentive Floating System Using Response Surface Methodology

Design and In Vitro Performance Evaluation of Purified Microparticles of Pravastatin Sodium for Intestinal Delivery

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