Preparation and in vitro/in vivo evaluation of nano-sized crystals for dissolution rate enhancement of ucb-35440-3, a highly dosed poorly water-soluble weak base

Hecq, Julien; Deleers, Michel; Fanara, D.; Vranckx, Henri; Boulanger, Philippe; Lamer, Sophie Le; Amighi, Karim

doi:10.1016/j.ejpb.2006.05.008

Cited by 81 publications

(37 citation statements)

References 11 publications

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“…Basically, such nanomedicines consist of DNCs dispersed in liquid medium, and are stabilized by surface-active agents, such as the poloxamer family, [169][170][171][172][173] Tween, [174][175][176] and polymers. [177][178][179][180] For oral administration, the high surface:volume ratios of DNCs significantly increase dissolution velocity, thereby leading to an improvement in the gastrointestinal tract absorption based on the Noyes-Whitney equation. 181 For intravenous administration, the smallness of this nanomedicine enables it to enter blood circulation and achieve targeted delivery through further surface modification.…”

Section: Drug Nanocrystalsmentioning

confidence: 99%

High drug-loading nanomedicines: progress, current status, and prospects

Shen

Liu

et al. 2017

IJN

412

268

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Drug molecules transformed into nanoparticles or endowed with nanostructures with or without the aid of carrier materials are referred to as “nanomedicines” and can overcome some inherent drawbacks of free drugs, such as poor water solubility, high drug dosage, and short drug half-life in vivo. However, most of the existing nanomedicines possess the drawback of low drug-loading (generally less than 10%) associated with more carrier materials. For intravenous administration, the extensive use of carrier materials might cause systemic toxicity and impose an extra burden of degradation, metabolism, and excretion of the materials for patients. Therefore, on the premise of guaranteeing therapeutic effect and function, reducing or avoiding the use of carrier materials is a promising alternative approach to solve these problems. Recently, high drug-loading nanomedicines, which have a drug-loading content higher than 10%, are attracting increasing interest. According to the fabrication strategies of nanomedicines, high drug-loading nanomedicines are divided into four main classes: nanomedicines with inert porous material as carrier, nanomedicines with drug as part of carrier, carrier-free nanomedicines, and nanomedicines following niche and complex strategies. To date, most of the existing high drug-loading nanomedicines belong to the first class, and few research studies have focused on other classes. In this review, we investigate the research status of high drug-loading nanomedicines and discuss the features of their fabrication strategies and optimum proposal in detail. We also point out deficiencies and developing direction of high drug-loading nanomedicines. We envision that high drug-loading nanomedicines will occupy an important position in the field of drug-delivery systems, and hope that novel perspectives will be proposed for the development of high drug-loading nanomedicines.

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Section: Drug Nanocrystalsmentioning

confidence: 99%

High drug-loading nanomedicines: progress, current status, and prospects

Shen

Liu

et al. 2017

IJN

412

268

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“…O fármaco pouco solúvel fica na interface o/a. 1,17 Esta tecnologia já foi utilizada no preparado de formulações intravenosas de diversos fármacos como, por exemplo, a anfotericina B (estrutura d), itraconazol (estrutura e), cetoconazol (estrutura f), carbamazepina 18 (estrutura g), cetoprofeno 19 (estrutura h), nifedipina 20 (estrutura i), ucb-35440-3 21 (estrutura j), hidrocortisona (estrutura k), prednisolona (estrutura l) ou dexametasona 22 (estrutura m), acetato de hidrocortisona 23,24 (estrutura n). A obtenção de nanoemulsões com a maioria destes compostos é complicada devido à baixa solubilidade dos mesmos.…”

Section: Tecnologia Solemuls ®unclassified

Tecnologia de nanocristais em fármacos

Durán¹,

Tasić²,

Marcato³

2010

Quím. Nova

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Recebido em 22/10/08; aceito em 28/5/09; publicado na web em 8/12/09 NANOCRYSTAL TECHNOLOGY IN PHARMACEUTICALS. The use of poorly water soluble molecules in pharmaceutical area has grown. Since these molecules exhibit low oral bioavailability, they are not used in intravenous administrations. Therefore, it is necessary to develop their new formulations with the aim to increase their oral bioavailabilities as to enable intravenous applications. One of the few possibilities in achieving this is a nanonization process that can produce crystals smaller than 1 mm by high pressure homogenization and without use of organic solvents. This mini-review describes technical aspects of the nanocrystal production, morphological aspects (polymorphisms), the market relevance of the nanocrystals products that are already in clinical phase or at the market, as well as, perspectives for the near future.Keywords: drugs; homogenization; nanocrystals. INTRODUÇÃODependendo da sua solubilidade em água, cada fármaco possui um perfil diferente e único de liberação e de ação no alvo. Os fármacos pouco solúveis em água, assim como os que apresentam sérios efeitos colaterais, requerem uma tecnologia para a sua liberação em um alvo-específico. Outros problemas como lenta absorção e a aplicação de volumes excessivos em administrações intravenosas (IV) podem ser melhorados através do uso de sistemas de liberação sustentada (sistemas inteligentes). 1 Isto ampliaria o uso de vários fármacos, alguns deles biotecnológicos, tais como a afidicolina (estrutura a), a violaceína (estrutura b) e o P-MAPA (estrutura c) . 2-5Os fármacos pouco solúveis em sistema aquosos 6 e, também, pouco solúveis em alguns meios orgânicos como, por exemplo, óle-os podem ser "solubilizados" em uma emulsão óleo em água (o/a). Neste caso, o fármaco pode se localizar na interface o/a. Baseado neste conceito, Muller 7 desenvolveu uma tecnologia livre de solvente capaz de incorporar fármacos na camada interfacial de emulsões óleo em água. Esta tecnologia, denominada de SolEmuls ® , 1 se baseia na co-homogeneização de cristais de fármacos adicionados a uma emulsão parenteral.Um outro problema de fármacos pouco solúveis em meio aquoso é a sua baixa biodisponibilidade quando administrados oralmente. Este fato pode ser atribuído a dois fatores, além da sua possível degradação no aparelho digestivo: baixa velocidade de dissolução e, baixa permeabilidade do fármaco nas paredes do aparelho digestivo. Em geral, fármacos que possuem baixa solubilidade apresentam também uma baixa velocidade de dissolução. Isto pode ser explicado pela Equação de Noyes-Whitney 8 que descreve a velocidade de dissolução (dc/dt) que é proporcional ao gradiente de concentração (c s -c x /h), onde o fator c s é a concentração total do fármaco no líquido (solubilidade de saturação) e o fator h é a distância de difusão acima da superfície da partícula do fármaco. A velocidade de dissolução é dada em função da área superficial: dc/dt = DA(c s − c x )/h onde D é o coeficiente de difusão e A é a área superficial. Q...

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“…The name of drugs and the relevant references are given in Table 1 (9)(10)(11)(12)(13)(14)(15)(16)(17)(18)(19)(20)(21)(22)(23)(24)(25)(26)(27). As seen in the table the data includes several kind of nanosystems intended for administration via different routes.…”

Section: Datamentioning

confidence: 99%

A Correlative Model to Predict In Vivo AUC for Nanosystem Drug Delivery with Release Rate-Limited Absorption

Barzegar-Jalali

Mohammadi

et al. 2012

J Pharm Pharm Sci

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-Purpose. Drug release from nanosystems at the sites of either absorption or effect biophase is a major determinant of its biological action. Thus, in vitro drug release is of paramount importance in gaining insight for the systems performance in vivo. Methods. A novel in vitro in vivo correlation, IVIVC, model denoted as double reciprocal area method was presented and applied to 19 drugs from 55 nano formulations with total 336 data, gathered from literature.Results. The proposed model correlated the in vitro with in vivo parameters with overall error of 12.4 ± 3.9%. Also the trained version of the model predicted the test formulations with overall error of 15.8 ± 3.7% indicating the suitability of the approach. A theoretical justification was provided for the model considering the unified classical release laws. Conclusion. The model does not necessitate bolus intravenous drug data and seems to be suitable for IVIVC of drugs with release rate-limited absorption.

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Preparation and in vitro/in vivo evaluation of nano-sized crystals for dissolution rate enhancement of ucb-35440-3, a highly dosed poorly water-soluble weak base

Cited by 81 publications

References 11 publications

High drug-loading nanomedicines: progress, current status, and prospects

High drug-loading nanomedicines: progress, current status, and prospects

Tecnologia de nanocristais em fármacos

A Correlative Model to Predict In Vivo AUC for Nanosystem Drug Delivery with Release Rate-Limited Absorption

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