Preparation and Characterization of Microemulsion of Cilostazol for Enhancement of Oral Bioavailability

Patel, Samir; Rajput, Sadhana J.; Groshev, Anastasia; Sutariya, Vijaykumar

doi:10.2174/1567201810666131126161957

Cited by 7 publications

(4 citation statements)

References 29 publications

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“…The heparinized blood samples were immediately collected in centrifugation tubes (5 mL) and centrifuged at 20000 rpm at 0°C for 15 minutes. Supernatant layer of plasma was separated into another centrifugation tube and stored at −20°C until analysis [ 7 ].…”

Section: Methodsmentioning

confidence: 99%

In Vitro Intestinal Permeability Studies and Pharmacokinetic Evaluation of Famotidine Microemulsion for Oral Delivery

Jha¹,

Karki

Puttegowda

et al. 2014

International Scholarly Research Notices

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The absolute bioavailability of famotidine after oral administration is about 40–45% and absorbance only in the initial part of small intestine may be due to low intestinal permeability. Hence, an olive oil based microemulsion formulation with Tween-80 as surfactant and PEG-400 as cosurfactant was developed by using water titration method with the aim of enhancing the intestinal permeability as well as oral bioavailability. In vitro drug permeation in intestine after 8 h for all formulations varied from 30.42% to 78.39% and most of the formulations showed enhanced permeation compared to pure drug (48.92%). Famotidine microemulsion exhibited the higher absorption and C max⁡ achieved from the optimized famotidine formulation (456.20 ng·h/ml) was higher than the standard (126.80 ng·h/mL). It was found that AUC0–24 h obtained from the optimized famotidine test formulation (3023.5 ng·h/mL) was significantly higher than the standard famotidine (1663.3 ng·h/mL). F-1 demonstrated a longer (6 h) T max⁡ compared with standard drug (2 h) and sustained the release of drug over 24 h. The bioavailability of F-1 formulation was about 1.8-fold higher than that of standard drug. This enhanced bioavailability of famotidine loaded in microemulsion system might be due to increased intestinal permeability.

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Section: Methodsmentioning

confidence: 99%

In Vitro Intestinal Permeability Studies and Pharmacokinetic Evaluation of Famotidine Microemulsion for Oral Delivery

Jha¹,

Karki

Puttegowda

et al. 2014

International Scholarly Research Notices

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“…Supernatant layer of plasma was separated into another centrifugation tube and stored at −20 ∘ C until analysis [5]. …”

Section: Pharmacokinetics Studymentioning

confidence: 99%

Pharmacodynamics and Pharmacokinetics Evaluation of Ranitidine Microemulsion on Experimental Animals

Jha¹,

Karki²,

Puttegowda³

et al. 2014

Advances in Pharmaceutics

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Ranitidine microemulsion was investigated for its pharmacodynamic and pharmacokinetic evaluation to find out the suitability of microemulsion as a potential drug delivery system in the treatment of ulcer. The bioavailability of ranitidine after oral administration is about 50% and is absorbed via the small intestine; this may be due to low intestinal permeability. Hence the aim of present investigation was to maximize the therapeutic efficacy of ranitidine by developing microemulsion to increase the intestinal permeability as well as bioavailability. A ground nut oil based microemulsion formulation with Tween-80 as surfactant and PEG-400 as cosurfactant was developed for oral delivery of ranitidine and characterized for physicochemical parameters. In pharmacodynamic studies, significant ( < 0.05) variation in parameters estimated was found between the treated and control groups. Ranitidine microemulsion exhibited higher absorption and C max (863.20 ng⋅h/mL) than the standard (442.20 ng/mL). It was found that AUC 0−24 hr obtained from the optimized ranitidine test formulation (5426.5 ng⋅h/mL) was significantly higher than the standard ranitidine (3920.4 ng⋅h/mL). The bioavailability of optimized formulation was about 1.4-fold higher than that of standard drug. This enhanced bioavailability of ranitidine microemulsion may be used as an effective and alternative drug delivery system for the antiulcer therapy.

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“…Among several strategies adapted to improve bioavailability, the major concern has always been on enhancing drug's water solubility 1,4,5 . Solubility of the active pharmaceutical ingredient (API) in the gastric medium is of prime significance as its fair absorption through the intestine and its bioavailability depends on this property.…”

Section: Introductionmentioning

confidence: 99%

Microemulsion Based Formulation as Drug Delivery System for Gliclazide

Kamath¹,

Sivakumar²

2017

IJPER

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Purpose: The present study is intended to develop and evaluate oil in water (O/W) microemulsion based formulation for gliclazide as oral drug delivery system for the treatment of diabetes mellitus. Gliclazide, having sulphonyl urea moiety (Class II of BCS system) is a hydrophobic drug. Methods: Oil in water microemulsion was formulated using water titration method. Viscosity, pH, conductivity, particle size and thermodynamic stability studies were carried out for optimization followed by In vitro drug release and in vivo pharmacokinetic study. Results: The formulated O/W microemulsion had olive oil, tween 80 and propylene glycol as ingredients with an average particle size 14.3 nm. The developed formulation showed a drug release of 82.4% while the pure drug in powdered form showed a release of 32.19% as observed through in vitro drug release studies. The data obtained by these studies was fitted to zero order, first order Higuchi and Korsmeyer Pappas models. The in vivo pharmacokinetic parameters of the optimized microemulsion was significantly (P<0.05) different when compared to the conventional tablet formulation. The peak serum concentration (C max ) for the microemulsion (2.998±0.419 μg/mL) was higher than that for the conventional tablet (2.118±0.169μg/mL), and the time required to reach the peak serum concentration (T max ) was significantly shorter for the optimized microemulsion (2.5±0.548 h) compared to the tablet formulation (5.333±1.033h). Conclusion: Gliclazide O/W microemulsion was found to be stable and showed superior in vitro and in vivo release. The study promises improved clinical efficacy for gliclazide as O/W microemulsion in the management of type 2 diabetes.

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Preparation and Characterization of Microemulsion of Cilostazol for Enhancement of Oral Bioavailability

Cited by 7 publications

References 29 publications

In Vitro Intestinal Permeability Studies and Pharmacokinetic Evaluation of Famotidine Microemulsion for Oral Delivery

In Vitro Intestinal Permeability Studies and Pharmacokinetic Evaluation of Famotidine Microemulsion for Oral Delivery

Pharmacodynamics and Pharmacokinetics Evaluation of Ranitidine Microemulsion on Experimental Animals

Microemulsion Based Formulation as Drug Delivery System for Gliclazide

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