Novel gastroretentive sustained-release tablet of tacrolimus based on self-microemulsifying mixture: in vitro evaluation and in vivo bioavailability test

Wang, Yanping; Gan, Yong; Zhang, Xinxin

doi:10.1038/aps.2011.90

Cited by 31 publications

(18 citation statements)

References 35 publications

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“…colloidal silica and magnesium stearate and compression force on hardness and dissolution of controlled release tablet of coenzyme Q10. It was also found that the solid carriers and compression force were in optimum level [76]. Tacrolimus was developed as gastroretentive SR tablet by using polyethylene oxide, chitosan, poly(vinyl pyrollidone) and mannitol as solid carrier.…”

Section: Recent Advancements In Seddsmentioning

confidence: 99%

Self Emulsifying Drug Delivery System: A Recent Approach

Bindhani

Mohapatra

Kar³

2019

Asian J. Chem.

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In recent years, nearly 40 % newer drugs compounds are hydrophobic in nature, which is a major challenge now-a-days for oral drug delivering due to low aqueous solubility. Lipid based drug delivery system is one of the favourable approach for poorly soluble compounds which can improve the drug absorption and oral bioavailability. Due to ion-pairing with appropriate surfactant and co-surfactant the macromolecular drug molecular oil droplet being found in the gut flow oral absorption which sufficiently stable towards lipase. Due to the formation of emulsified drug in micron level, it can efficiently endow the oral bioavailability. Several comprehensive papers have been published in the literature illustration diverse type of lipid based formulation with recent advancements. This article is based on an exhaustive and updated review on newer technology which out line an explicit discussion on its formulations and industrial scale up.

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Section: Recent Advancements In Seddsmentioning

confidence: 99%

Self Emulsifying Drug Delivery System: A Recent Approach

Bindhani

Mohapatra

Kar³

2019

Asian J. Chem.

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“…Wang et al .,[32] developed a novel gastro-retentive drug delivery system based on a self-microemulsifying (SME) lipid mixture for improving the oral absorption of the immunosuppressant tacrolimus. Liquid SME mixture composed of Cremophor RH40 and monocaprylinglycerate, was blended with polyethylene oxide, chitosan, polyvinylpyrrolidone, and mannitol, and then transformed into tablets via granulation, with ethanol as the wetting agent.…”

Section: Tacrolimus Drug Delivery Systemsmentioning

confidence: 99%

Formulation strategies for drug delivery of tacrolimus: An overview

Patel¹,

Patel²,

Panchal

et al. 2012

Int J Pharma Investig

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Tacrolimus (FK 506) is a potent macrolide lactone immunosuppressive agent used for prophylaxis of organ rejection after transplantation and graft-versus-host disease after bone marrow transplantation in patients. Moreover, tacrolimus is a drug of choice in the treatment of atopic dermatitis for decreasing side effects associated with the use of topical corticosteroids. In spite of its success in ensuring graft survival, therapeutic use of tacrolimus is complicated due to its narrow therapeutic index (between 5 and 15 ng/ml). Tacrolimus has a large inter-/intra-patient variability in pharmacokinetics profile and a poor oral bioavailability because of its poor solubility, P-gp efflux, marked pre-systemic metabolism by CYP3A in the enterocytes and liver first pass effect. Several formulation approaches such as oily solution, solid dispersions, complexation with cyclodextrins, liposomes etc., have been investigated to improve oral delivery of FK 506. In this review, we have discussed various formulation approaches that have been undertaken by various researchers to solve the problems related to the drug delivery of tacrolimus.

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“…Tacrolimus is also a drug of choice for atopic dermatitis in reducing the side effects related with topical corticosteroids. Tacrolimus is classified as a class II drug according to the biopharmaceutical classification system (12). Tacrolimus exhibits poor aqueous solubility, P-gp efflux, and extensive presystemic metabolism resulting in low bioavailability following oral administration (13)(14)(15)(16).…”

Section: Introductionmentioning

confidence: 99%

Design, Characterization, and In Vivo Pharmacokinetics of Tacrolimus Proliposomes

et al. 2015

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Abstract. The objective of this study was to develop proliposomal formulation for a poorly bioavailable drug, tacrolimus. Proliposomes were prepared by thin film hydration method using different lipids such as hydrogenated soy phosphatidylcholine (HEPC), soy phosphatidylcholine (SPC), distearyl phosphatidylcholine (DSPC), dimyristoylphosphatidylcholine (DMPC), and dimyristoylphosphatidylglycerol sodium (DMPG) and cholesterol in various ratios. Proliposomes were evaluated for particle size, zeta potential, in vitro drug release, in vitro permeability, and in vivo pharmacokinetics. In vitro drug release was carried out in purified water using USP type II dissolution apparatus. In vitro drug permeation was studied using parallel artificial membrane permeation assay (PAMPA) and everted rat intestinal perfusion techniques. In vivo pharmacokinetic studies were conducted in male Sprague-Dawley (SD) rats. Among the different formulations, proliposomes with drug/DSPC/cholesterol in the ratio of 1:2:0.5 demonstrated the desired particle size and zeta potential. Enhanced drug release was observed with proliposomes compared to pure tacrolimus in purified water after 1 h. Tacrolimus permeability across PAMPA and everted rat intestinal perfusion models was significantly higher with proliposomes. The optimized formulation of proliposomes indicated a significant improvement in the rate and absorption of tacrolimus. Following a single oral administration, a relative bioavailability of 193.33% was achieved compared to pure tacrolimus suspension.

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Novel gastroretentive sustained-release tablet of tacrolimus based on self-microemulsifying mixture: in vitro evaluation and in vivo bioavailability test

Cited by 31 publications

References 35 publications

Self Emulsifying Drug Delivery System: A Recent Approach

Self Emulsifying Drug Delivery System: A Recent Approach

Formulation strategies for drug delivery of tacrolimus: An overview

Design, Characterization, and In Vivo Pharmacokinetics of Tacrolimus Proliposomes

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