Swelling of and Drug Release from Monoglyceride-Based Drug Delivery Systems

Chang, Chin-Ming; Bodmeier, Roland

doi:10.1021/js960256w

Cited by 110 publications

(77 citation statements)

References 24 publications

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“…In the previous report about cubosomal preparation, drug usually was added into the melted PYT or Glyceryl monooleate (GMO) and stirred continuously till the complete dissolution (14,23,24). To date, nothing has been done to improve the poor solubility of drug in PYT or GMO for developing cubosomal formulations.…”

Section: Discussionmentioning

confidence: 99%

Development of Amphotericin B-Loaded Cubosomes Through the SolEmuls Technology for Enhancing the Oral Bioavailability

et al. 2012

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Abstract. The oral administration of amphotericin B (AmB) has the major drawback of poor bioavailability. The aim of this work was to evaluate the potential of AmB-loaded cubosomes as an oral formulation with improved bioavailability. This manuscript firstly developed AmB-loaded cubosomes by using the SolEmuls technology. The encapsulation efficiency, the in vitro release, and stability studies in simulated gastrointestinal fluid were used to evaluate AmB-loaded cubosomes. The acute nephrotoxicity, bioavailability, and tissue distribution study of AmB-loaded cubosomes were assayed upon oral administration to rats. SAXS and cryo-TEM exhibited AmB-loaded cubosomes as a bicontinuous cubic liquid crystalline phase with Pn3m geometry. The encapsulation efficiency and the results of in vitro release and stability studies in simulated gastrointestinal fluid further demonstrated that AmB was successfully encapsulated in cubosomes. AmB-loaded cubosomal formulation orally administrated in rats did not show nephrotoxicity and its relative bioavailability was approximately 285% as compared to Fungizone®. The AmB-loaded cubosomal formulation presented an effective potential approach for enhancing the oral bioavailability of AmB.

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Section: Discussionmentioning

confidence: 99%

Development of Amphotericin B-Loaded Cubosomes Through the SolEmuls Technology for Enhancing the Oral Bioavailability

et al. 2012

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“…Monoolein absorbs water in the presence of excess water until its maximum water content is reached (approximately 40.0% w/w), after which it adopts a cubic phase. It is suggested that this water uptake is rapid and that drug release occurs primarily from the cubic phase formed (40). The liquid crystalline systems evaluated in this study showed rapid water uptake and the very quick transition to the cubic phase.…”

Section: Discussionmentioning

confidence: 66%

“…Cubic phases are reported to provide a slow release matrix for the incorporated drugs, and therefore, they are largely used as drug delivery systems for several routes of administration (19,20,23,40). This liquid crystalline phase is thermodynamically stable and macroscopically stiff, and it consists of one congruent lipid bilayer that extends in three dimensions, surrounded by water channels (9,14).…”

Section: Discussionmentioning

confidence: 99%

“…The release profiles of several drugs from monoolein/water systems were reported as a linear function with the square root of time, which indicates a diffusion-controlled release (25,31,(39)(40)(41)(42)(43). However, when the dissolution of a drug is the rate-limiting step for drug release, the release data can follow zero-order kinetics (30).…”

Section: Discussionmentioning

confidence: 99%

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Liquid Crystalline Systems for Transdermal Delivery of Celecoxib: In Vitro Drug Release and Skin Permeation Studies

et al. 2014

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Abstract. Liquid crystalline systems of monoolein/water could be a promising approach for the delivery of celecoxib (CXB) to the skin because these systems can sustain drug release, improve drug penetration into the skin layers and minimize side effects. This study evaluated the potential of these systems for the delivery of CXB into the skin based on in vitro drug release and skin permeation studies. The amount of CXB that permeated into and/or was retained in the skin was assayed using an HPLC method. Polarizing light microscopy studies showed that liquid crystalline systems of monoolein/water were formed in the presence of CXB, without any changes in the mesophases. The liquid crystalline systems decreased drug release when compared to control solution. Drug release was independent of the initial water content of the systems and CXB was released from cubic phase systems, irrespective of the initial water content. The systems released the CXB following zero-order release kinetics. In vitro drug permeation studies showed that cubic phase systems allowed drug permeation and retention in the skin layers. Cubic phase systems of monoolein/water may be promising vehicles for the delivery of CXB in/through the skin because it improved CXB skin permeation compared with the control solution.

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“…Sodium deoxycholate (Na-DOC), was proposed as an alternative to polymeric matrices for developing drug carrier systems [1][2][3]. Na-DOC is a low molecular weight polymer (414.5) with advantages as low melt viscosity, potential biocompatibility, biodegradability and the absence of toxic impurities [4] (Valenta et al, 1999).…”

Section: Introductionmentioning

confidence: 99%

Gelation of Sodium-Deoxycholate: Influenced by the Presence of a CorticosteroidBetamethasone-17-Valerate

Homan¹

2017

J. Drug

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This study was designed to evaluate the possible influences of betamethasone-17-valerate (BMV) on the gelation properties of sodium deoxycholate (Na-DOC), due to structural similarities as the monomer and the active agent. For this purpose gel formulations at two different concentrations, 0.05 and 0.1 % (w/w) were prepared and characterized by rheological and thermal analysis. The results indicated that the elastic moduli of the gels increased with increasing concentration of BMV in the system. This phenomenon was shown to be due to the modification of polymerization occurred by interactions between BMV and Na-DOC. The increment of BMV concentration in the formulation, caused a modification of the glass transition temperature (Tg) detected. Tg data pointed out a higher polymerization of Na-DOC with increasing amount of BMV. Transepidermal water loss measurements were also performed to evaluate possible skin irritation. It was observed that the degree of Na-DOC polymerization did not show any irritant effect on the skin.Overall, the results of this study clearly confirmed that incorporation of BMV into Na-DOC gel system produced a synergistic effect on product rheological characteristics, which would be beneficial for topical applications.

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Swelling of and Drug Release from Monoglyceride-Based Drug Delivery Systems

Cited by 110 publications

References 24 publications

Development of Amphotericin B-Loaded Cubosomes Through the SolEmuls Technology for Enhancing the Oral Bioavailability

Development of Amphotericin B-Loaded Cubosomes Through the SolEmuls Technology for Enhancing the Oral Bioavailability

Liquid Crystalline Systems for Transdermal Delivery of Celecoxib: In Vitro Drug Release and Skin Permeation Studies

Gelation of Sodium-Deoxycholate: Influenced by the Presence of a CorticosteroidBetamethasone-17-Valerate

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