Development of microemulsion of mitotane for improvement of oral bioavailability

Attivi, David; Ajana, Imane; Astier, A.; Demoré, Béatrice; Gibaud, Stéphane

doi:10.1080/03639040903225083

Cited by 5 publications

(7 citation statements)

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“…It has been reported that the drug incorporated into an O/W microemulsion (i.e., The Ussing chamber method has been used to compare the absorption of O/W microemulsions of mitotane with crystals of mitotane [16]. However, the results of the Ussing test indicated that this comparison would require in vivo testing.…”

Section: Everted Sac and Ussing Chambermentioning

confidence: 99%

Microemulsions for oral administration and their therapeutic applications

Gibaud

Attivi²

2012

Expert Opinion on Drug Delivery

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Actual applications of S(M)EDDS remain rare. The first drug marketed as a S(M)EDDS was cyclosporin, and it had significantly improved bioavailability compared with the conventional solution. In the last decade, several S(M)EDDS loaded with antiviral drugs (e.g., ritonavir, saquinavir) were tested for treatment of HIV infection, but the relative improvement in clinical benefit was not significant. The S(M)EDDS formulation of Norvir® (soft capsules) has been withdrawn in some countries.

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Section: Everted Sac and Ussing Chambermentioning

confidence: 99%

Microemulsions for oral administration and their therapeutic applications

Gibaud

Attivi²

2012

Expert Opinion on Drug Delivery

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“…The LT and cosurfactant were combined at 1:2, 1:1, and 2:1 weight ratios, then mixed with IPM as oil phase at certain weight ratios (1/9, 2/8, 3/7, 4/6, 5/5, 6/4, 7/3, 8/2 and 9/1, w/w), and titrated with water in a dropwise manner under magnetic agitation, until the mixture became clear and flowable at a certain point. 24,32 The concentrations of components were recorded to construct the pseudoternary phase diagrams.…”

Section: Construction Of Ternary Phase Diagramsmentioning

confidence: 99%

“…[11][12][13][14][15][16][17][18][19] Nanoemulsion formulations have been widely used to overcome problems related to the poor water solubility and low oral bioavailability of some drugs. [20][21][22][23][24][25][26] Therefore, amongst the various drug delivery systems, nanoemulsions are considered an ideal alternative for the oral administration of drugs with poor water solubility, as they improve absorption and bioavailability. At present, the US Food and Drug Administration has approved nanoemulsions of compounds with poor water solubility, including cyclosporin (Neoral ® , Gengraf ® ), 27,28 saquinavir (Fortovase ® ), 29,30 and ritonavir (Norvir ® ), 31 for clinical use.…”

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confidence: 99%

Nanoemulsion improves the oral bioavailability of baicalin in rats: in vitro and in vivo evaluation

Zhao¹,

Wei²,

Huang³

et al. 2013

IJN

112

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“…Among emerging technologies (i.e. self-microemulsifying drug delivery system (SMEDDS) for mitotane [71]), nanotechnology using nano-carriers for drug delivery could offer tremendous possibilities to improve efficacy and significantly decrease the side effects associated with drug hydrophobicity which, in turn can compromise the drug bioavailability, safety and efficacy (i.e. disease targeting).…”

Section: Mitotane Nano-formulations: From Concept To Developmentmentioning

confidence: 99%

Development of Mitotane Lipid Nanocarriers and Enantiomers: Two-in-One Solution to Efficiently Treat Adreno-Cortical Carcinoma

Menaa¹,

Menaa²

2012

CMC

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Adrenocortical carcinoma (ACC) is a rare but aggressive malignancy with a poor prognosis. Treatment options for advanced ACC are limited. Indeed, radical tumor resection can lead to local or metastatic recurrence, and mitotane (Lysodren(®)), the only recognized adrenolytic drug, offers modest response rates, notably due to some of its physico-chemical and pharmacological properties (i.e. hydrophobicity, low bioavailability). Meantime, high cumulative doses of Lysodren(®) usually cause systemic toxicities. To reduce adverse health effects, the search of safe and efficient mitotane nano-formulations as well as the full characterization and testing of its enantiomers can represent valuable therapeutic options. Interestingly, recent investigations showed that solid lipid nanoparticles (SLN) and nanostructured lipid carriers (NLC) could considerably improve the efficacy of mitotane (i.e. enhanced solubility and bioavailability, progressive release of the loaded drug into blood and targeted tissues) as well as its safety (i.e. lower toxicity, higher biocompatibility). These two nano-carriers for mitotane delivery and targeting are of particular interest over other polymeric particles (i.e. low-cost, efficient and simple scaling to an industrial production level following green methods). Besides, emerging studies suggested that the S-(-)- mitotane is more potent than the R-(+)-mitotane for ACC treatment. Therefore, the production of pure and active S-(-)-mitotane might offer synergic or additive benefits for ACC patients when combined to solid lipid-based nanocarriers. In this review, we first provide an updated overview of the ACC disease before emphasizing on the promising mitotane drug nano-systems, as well as on the separation, purification and production of single mitotane enantiomer using state-of-art chromatographic-based methods.

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Development of microemulsion of mitotane for improvement of oral bioavailability

Cited by 5 publications

References 0 publications

Microemulsions for oral administration and their therapeutic applications

Microemulsions for oral administration and their therapeutic applications

Nanoemulsion improves the oral bioavailability of baicalin in rats: in vitro and in vivo evaluation

Development of Mitotane Lipid Nanocarriers and Enantiomers: Two-in-One Solution to Efficiently Treat Adreno-Cortical Carcinoma

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