Tricaprylin microemulsion for oral delivery of low molecular weight heparin conjugates

Kim, Sang Kyoon; Lee, Eun Hye; Bagalkot, Vaishali; Lee, Seulki; Lee, Yong-Kyu; Kim, Choong-Yong; Moon, Hyun Tae; Byun, Youngro

doi:10.1016/j.jconrel.2005.03.018

Cited by 59 publications

(39 citation statements)

References 27 publications

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“…The ability to formulate such mixtures with biocompatible ingredients has made possible to use them in biological and health related areas extensively. Hence, microemulsions have found wide application in delivering drugs with different physical and chemical characteristics and different ways of delivering such as, oral delivery of protein drugs (Sarciaux et al, 1995, Ke et al, 2005, Cheng et al, 2008, Kim et al, 2005, ophthalmic (Lv et al, 2005., Gulsen & Chauhan, 2005, transdermal (Kantaria et al, 1999, Kreilgaard et al, 2000, Sintov & Botner 2006, Neubert, 2011, Zhu et al, 2008, amphiphilic drugs (Djordjevic et al, 2004, Oh et al, 2011, internasal (Cho et al, 2012) or other ways (Zhou et al, 2011, Lawrence & Rees, 2000.…”

Section: Applications In Biological and Health Sciencesmentioning

confidence: 99%

Microemulsions - A Brief Introduction

Najjar¹

2012

Microemulsions - An Introduction to Properties and Applications

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Section: Applications In Biological and Health Sciencesmentioning

confidence: 99%

Microemulsions - A Brief Introduction

Najjar¹

2012

Microemulsions - An Introduction to Properties and Applications

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“…Oilin-water microemulsions are promising in improving the bioavailability of hydrophobic molecules, including hydrophobic peptides, such as cyclosporine A (12). Water-in-oil microemulsions, on the other hand, have shown potential to improve the oral delivery of hydrophilic peptides or proteins (10,11,13,14). The mechanisms proposed for improved bioavailability using w/o microemulsions were based on increased protection from luminal enzymatic degradation and/or enhancer-induced structural and fluidity changes in the mucosal membrane (13,15,16).…”

Section: Introductionmentioning

confidence: 99%

“…The mechanisms proposed for improved bioavailability using w/o microemulsions were based on increased protection from luminal enzymatic degradation and/or enhancer-induced structural and fluidity changes in the mucosal membrane (13,15,16). The safety evaluation of several orally delivered w/o microemulsions has been investigated (10,11,14), and histological examination showed no intestinal tissue damage or irritation upon acute dosing of the specific vehicles.…”

Section: Introductionmentioning

confidence: 99%

“…Based on some prior research results (10,11,13,14), w/o microemulsions were developed using several commercially available and pharmaceutically acceptable lipid-based excipients. Miglyol 812 and Capmul MCM are medium-chain (C 8 / C 10 ) glycerides, generally recognized as safe, and meet the requirements of the United States Pharmacopeia (USP) and The National Formulary as medium-chain triglycerides and mono-and di-glycerides (18,19), respectively.…”

Section: Introductionmentioning

confidence: 99%

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In Vitro and In Vivo Evaluation of a Water-in-Oil Microemulsion System for Enhanced Peptide Intestinal Delivery

Liu

Russo

et al. 2012

AAPS J

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Abstract. Peptide and protein drugs have become the new generation of therapeutics, yet most of them are only available as injections, and reports on oral local intestinal delivery of peptides and proteins are quite limited. The aim of this work was to develop and evaluate a water-in-oil (w/o) microemulsion system in vitro and in vivo for local intestinal delivery of water-soluble peptides after oral administration. A fluorescent labeled peptide, 5-(and-6)-carboxytetramethylrhodamine labeled HIV transactivator protein TAT (TAMRA-TAT), was used as a model peptide. Water-in-oil microemulsions consisting of Miglyol 812, Capmul MCM, Tween 80, and water were developed and characterized in terms of appearance, viscosity, conductivity, morphology, and particle size analysis. TAMRA-TAT was loaded and its enzymatic stability was assessed in modified simulated intestinal fluid (MSIF) in vitro. In in vivo studies, TAMRA-TAT intestinal distribution was evaluated using fluorescence microscopy after TAMRA-TAT microemulsion, TAMRA-TAT solution, and placebo microemulsion were orally gavaged to mice. The half-life of TAMRA-TAT in microemulsion was enhanced nearly three-fold compared to that in the water solution when challenged by MSIF. The treatment with TAMRA-TAT microemulsion after oral administration resulted in greater fluorescence intensity in all intestine sections (duodenum, jejunum, ileum, and colon) compared to TAMRA-TAT solution or placebo microemulsion. The in vitro and in vivo studies together suggested TAMRA-TAT was better protected in the w/o microemulsion in an enzyme-containing environment, suggesting that the w/o microemulsions developed in this study may serve as a potential delivery vehicle for local intestinal delivery of peptides or proteins after oral administration.

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“…18) Many researchers working on increasing the solubility of low-soluble drugs have focused on the formulation of lecithin-based microemulsions and studies have shown that microemulsions can be formulated using lecithin and a co-surfactant such as short-, medium-or long-chain alcohols. [18][19][20] Microemulsions were also used to stabilize active substances, 21,22) and to improve oral [23][24][25] availability of drugs. Microemulsions were shown to be effective dermal delivery mechanism for several active ingredients for pharmaceutical and cosmetic applications.…”

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confidence: 99%

Preparation and Evaluation of Topical Microemulsion System Containing Metronidazole for Remission in Rosacea

et al. 2012

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The aim of this study was to prepare a topical water-in-oil type microemulsion containing metronidazole and to compare its effectiveness with a commercial gel product in the treatment of rosacea. A pseudoternary phase diagram (K m 2 : 1) was constructed using lecithin/butanol/isopropyl myristate/water. The microemulsion was chosen from the microemulsion region in the phase diagram. The formulation was a water-in-oil type microemulsion (droplet size: 11.6 nm, viscosity: 457.3 mPa·s, conductivity: 1.5 µs/cm, turbidity: 6.89 NTU) and the addition of the metronidazole did not alter the properties of the system. The release experiment showed that the release rate of metronidazole from the commercial gel product was higher than that of the microemulsion. Stability experiments showed that the metronidazole microemulsion remained stable for at least 6 months; none of the characteristic properties of the microemulsion had changed, the system retained its clarity and there was no sign that crystallization of metronidazole has occurred. Microemulsion was compared to a gel product in a randomized, double-blind, baseline-controlled, split-face clinical trial for the treatment of patients. After the 6-week treatment period there was a statistically significant difference in reduction of the main symptoms of rosacea. Of the patients treated with the microemulsion, 17% experienced complete relief from inflammatory lesions, and 50% from erythema. The microemulsion resulted in complete relief in 38% of the patients with telangiectasia while the commercial product did not provide any relief of telangiectasia symptoms. In conclusion, the microemulsion containing metronidazole was found to be more effective in reducing the symptoms of rosacea compared to the commercial gel product. Key words microemulsion; metronidazole; rosaceaRosacea is a chronic skin disorder of unknown etiology that is more common in women than men.

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Tricaprylin microemulsion for oral delivery of low molecular weight heparin conjugates

Cited by 59 publications

References 27 publications

Microemulsions - A Brief Introduction

Microemulsions - A Brief Introduction

In Vitro and In Vivo Evaluation of a Water-in-Oil Microemulsion System for Enhanced Peptide Intestinal Delivery

Preparation and Evaluation of Topical Microemulsion System Containing Metronidazole for Remission in Rosacea

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