Enhanced bioavailability of lacidipine via microemulsion based transdermal gels: Formulation optimization, ex vivo and in vivo characterization

Gannu, Ramesh; Palem, Chinna Reddy; Yamsani, Vamshi Vishnu; Yamsani, Shravan Kumar; Yamsani, Madhusudan Rao

doi:10.1016/j.ijpharm.2009.12.050

Cited by 128 publications

(73 citation statements)

References 25 publications

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“…This also confirms the results of improved oral bioavailability for the FVSMs, which was supported by other studies on microemulsion. 36 Similar trend was also seen in the maximum concentration of ergosterol and 22,23-dihydroergosterol, which increased to about 2.78-fold and 5.16-fold, respectively, with FVSMs oral administration as against the free FVS. The improved oral bioavailability could be due to the predominant improved solubility of sterols in microemulsions which kept the drug in the soluble form during the gastrointestinal dilution and permeation process and the synergistic effect of oil and surfactants as absorption enhancers.…”

Section: In Vivo Studies Pharmacokinetics Of Fvsms In Ratssupporting

confidence: 64%

Enhanced oral bioavailability of a sterol-loaded microemulsion formulation of Flammulina velutipes, a potential antitumor drug

Yi¹,

Zhong²,

Tong³

et al. 2012

IJN

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Purpose:To investigate the growth inhibition activity of Flammulina velutipes sterol (FVS) against certain human cancer cell lines (gastric SGC and colon LoVo) and to evaluate the optimum microemulsion prescription, as well as the pharmacokinetics of encapsulated FVS. Methods: Molecules present in the FVS isolate were identified by gas chromatography/mass spectrometry analysis. The cell viability of FVS was assessed with methyl thiazolyl tetrazolium (MTT) bioassay. Based on the solubility study, phase diagram and stability tests, the optimum prescription of F. velutipes sterol microemulsions (FVSMs) were determined, followed by FVSMs characterization, and its in vivo pharmacokinetic study in rats. ). The optimal FVSMs prescription consisted of 3.0% medium chain triglycerides, 5.0% ethanol, 21.0% Cremophor EL and 71.0% water (w/w) with associated solubility of FVS being 0.680 mg ⋅ mL −1 as compared to free FVS (0.67 µg ⋅ mL −1 ). The relative oral bioavailability (area-under-the-curve values of ergosterol and 22,23-dihydroergosterol showed a 2.56-fold and 4.50-fold increase, respectively) of FVSMs (mean diameter ∼ 22.9 nm) as against free FVS were greatly enhanced. Our laboratory has been able to screen out lipid soluble sterols with an antitumor effect from F. velutipes by lipidraft chromatography, which was found to be linked to the tyrosine kinase receptor (data not published). In this study, our laboratory was interested in performing a preliminary investigation of the anticancer potential and bioavailability of F. velutipes sterol (FVS) as an in-depth contribution to the research of F. velutipes. FVS is a white powder, which can easily dissolve in ether, chloroform, hot ethanol, and other organic solvents, but barely dissolves in water. As a result, it is necessary to find a method to improve the solubility and oral bioavailability of this sterol. Dovepress 5067 O R I G I N A L R E S E A R C HMicroemulsions are thermodynamically stable nanometer systems with characteristics of easy preparation, small droplet size, low viscosity, and strong solubilization effect. 12It is formed spontaneously by water, oil, surfactant and cosurfactant. 13,14 According to the structure of a microemulsion, it can be divided into water-in-oil (w/o), oil-in-water (o/w) and bicontinuous microemulsion. 15 As a drug carrier, a microemulsion can increase the solubility and oral bioavailability of poorly soluble drugs, ameliorate the localization, improve systemic delivery of the drug, and possess the ability of targeting drug release. [16][17][18] The absolute bioavailability of a poorly soluble drug cyclosporin A which was loaded into a microemulsion system was increased to about 3.3-and 1.25-fold compared with free Sandimmun and Sandimmun Neoral (Novartis, Basel, Switzerland), which were used as commercial cyclosporin A. 19 In addition, it has been confirmed that the microemulsion system containing the poorly soluble drug docetaxel could improve the solubilization property and oral bioavailability of the drug. 20 Presently, there a...

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Section: In Vivo Studies Pharmacokinetics Of Fvsms In Ratssupporting

confidence: 64%

Enhanced oral bioavailability of a sterol-loaded microemulsion formulation of Flammulina velutipes, a potential antitumor drug

Yi¹,

Zhong²,

Tong³

et al. 2012

IJN

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“…The smaller the droplet size, the larger will be interfacial surface area provided for drug permeation. 21,27 Globule size of (F2) formulation was found to be 27.53 nm Table 2. The viscosity of optimized microemulsion (F2) was found to be 120 cps at 100 rpm which was determined by using Brookfield viscometer (DV II + PRO) with small sample volume adaptor.…”

Section: Evaluation Parameter For Microemulsionmentioning

confidence: 97%

Enhancement of Percutaneous Delivery of Dapsone by Microemulsion Gel

Mahore¹,

Suryawanshi²,

Shirolkar³

et al. 2017

JYP

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Objective: The purpose of this study was to developed microemulsion based gel formulation for topical delivery of dapsone with an objective to increase the solubility and skin permeability of the drug for treatment of acne. Methodology: The solubility of dapsone in oils, surfactants and cosurfactants was evaluated by saturation solubility to screen the components of the microemulsion. The pseudoternary phase diagrams were constructed using capryol 90 and N-methyl-2 pyrrolidone as the oil phase, Kolliphor EL as surfactant and PEG 400 as the co-surfactant. The system were assessed for drug-loading efficiency and characterized for pH, conductance, viscosity, particle size, drug content, globule size, zeta potential and drug release. Optimized formulation systems were formulated into gel form by using poloxamer-407 and evaluated for viscosity, spreadability, drug content, stability, in-vitro skin permeation, steady state flux, permeability coefficient, enhancement ration and skin irritation study. Result and Discussion: Globule size of optimized microemulsion (F2) was found to be 27.53 nm, zeta potential was found to be-14.6 mV, permeability of drug from microemulsion within 8h was observed 82%, In-vitro diffusion study showed increase in flux of microemulsion based gel (392.43 µg cm-2 h-1) to that of simple dapsone gel (274.4 ± 0.78 µg cm-2h-1). Draize test revealed absence of irritation and inflammation on rat skin. Conclusion: Microemulsion based gel of dapsone formulation provided better application property and stability in comparison to simple gel. This is an open access article distributed under the terms of the Creative Commons Attribution-NonCommercial-ShareAlike 4.0 License, which allows others to remix, tweak, and build upon the work non-commercially, as long as the author is credited and the new creations are licensed under the identical terms.

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“…Qs to 100 28.00 0.043 b 13 78.00 −9.750E-003 b 23 −7.75 0.062 b 11 18.13 −0.065 b 22 −46.12 0.11 b 33 5.37 0.065 It is expressed to understand the maximum surface area of the skin, in which the formulation spreads over. On the contrary, spread ability has a direct impact on drug distribution and penetration throughout the skin.…”

Section: Spread Ability Studiesmentioning

confidence: 99%

“…Moreover, it also improves nanoemulsion stability by declining the surface and interfacial tension and also increases the viscosity of the aqueous phase for proper drug administration. Nanoemulgel has addition advantages such as it is more adhere toward skin surface and leads to higher concentration gradients toward skin hence assured better penetration [12][13][14]. The nanoemulgel formulation has an outstanding thixotropic profile and has excellent spreadability and prominent thermodynamic stability.…”

Section: Introductionmentioning

confidence: 99%

Formulation and Optimization of Celecoxib Nanoemulgel

Bhattacharya

Prajapati

2017

Asian J Pharm Clin Res

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Objective: The main objective of this experiment was to prepare and optimized celecoxib nanoemulgel. This formulation can be used for acute rheumatoid arthritis patients. Methods:Celecoxib is a poorly water soluble drug. We prepared celecoxib nanoemulgel to improve intrinsic solubility of celecoxib and enhance deeper permeation throughout the skin. After several screening, the combination of acetonitrile, triacetin, campul 908P was considered for oil phase; acconon MC8-2EP as surfactant, and capmul MCM C-10 as a co-surfactant accordingly. As per Box-Behnken surface design model, optimization was done for all the 13 formulations.Results: Based on pseudo ternary plot, it was found that 4:1 S mix ratio was optimum and possessed maximum drug solubility. Further, screening shown, 0.25-0.75% carbopol-940 can be a stable candidate for hydrogel preparation. Prepared nanoemulsions and hydrogels were admixed to prepare nanoemulgel. Based on overlay plot, EG14* formulation was consider as optimum one, and various evaluation parameters were performed along with other formulations. Using Franz diffusion cell, in-vitro diffusion studies was performed. Almost all the formulations produces good qualitative drug release profile. The EG14* shown 95.50% drug release after 12 th hrs with standard Higuchi plot (R 2 value 0.9989). The optimum viscosity was found to be 521±0.81 mPas at 100 rpm. The appearance of the formulations was milky, yellowish white with expectable pH ranged from 5.8 to 6.7. The optimized formulation has good spreadability coefficient, good ex-vivo diffusion enhancement factor (3.03) as compare to marketed gel. Mostly, our formulations have less skin irritation and higher anti-inflammatory activity (92.56% of inhibition of paw edema for EG14*). Conclusion:From the thermodynamic studies, it was confirmed that EG14* maintained excellent stability profile in various heating-cooling cycle, centrifugation, and freeze-thaw cycle condition. Hence, it can be conclude that, our formulation, can be consider for pilot scale up.

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Enhanced bioavailability of lacidipine via microemulsion based transdermal gels: Formulation optimization, ex vivo and in vivo characterization

Cited by 128 publications

References 25 publications

Enhanced oral bioavailability of a sterol-loaded microemulsion formulation of Flammulina velutipes, a potential antitumor drug

Enhanced oral bioavailability of a sterol-loaded microemulsion formulation of Flammulina velutipes, a potential antitumor drug

Enhancement of Percutaneous Delivery of Dapsone by Microemulsion Gel

Formulation and Optimization of Celecoxib Nanoemulgel

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