Preparation and evaluation of nanosuspensions for enhancing the dissolution of poorly soluble drugs

Kocbek, Petra; Baumgartner, Stephan; Kristl, Julijana

doi:10.1016/j.ijpharm.2006.01.008

Cited by 336 publications

(211 citation statements)

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“…5. The choice of suitable stabilizers and its concentration are the most important factors to control the size and stability of the nanosuspension during nanoprecipitation methods [36,37] In our work; PVP-K30 was used at different concentration (table 1). The results showed that particle size is reduced with the increasing of stabilizer concentration as the particle size of formula F1 which contains 1:0.5 of drug: pvp-k30 ratio was 470.5±0.0 nm compared with 324.3±0.0 nm for F5 which contains 1:1 ratio of drug: stabilizer.…”

Section: The Particle Size and Pdi For Different Formulations Of Diffmentioning

confidence: 99%

Formulation and in Vitro Evaluation of Azilsartan Medoxomil Nanosuspension

Jassem

Rajab

2017

Int J Pharm Pharm Sci

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Objective: The objective of this study was to formulate and evaluate of the poorly soluble drug, azilsartan medoxomil into nanosuspension to increase the solubility and enhance the dissolution rate and then improve its bioavailability.Methods: Nanosuspension of azilsartan medoxomil was prepared using solvent-antisolvent precipitation method using PVP-K30 as a stabilizer. Eight formulations were prepared to show the effect of different parameters in which four formulations show the effect of stabilizer concentration, three formulations show the effect of stirring speed and two formulations prepare to show the effect of the addition of co-stabilizer such as sodium lauryl sulphate (SLS) and tween 80. All these formulation are evaluated for their particle size and entrapment efficiency. The selected one was evaluated for zeta potential, scanning electron microscope (SEM), saturation solubility, and in vitro drug release.Results: All the prepared formulations were in the nano size. The optimum concentration of the stabilizer was in the formulation when the drug: stabilizer ratio 1:1 and optimum stirring speed was 300 rpm. Dramatic effect on the particle size reduction was found by the addition of costabilizer (SLS) in formulation F3 that has P. S 157±0.0 nm. The selected formula F3 showed an enhanced dissolution profile compared to the pure drug at all-time intervals. Conclusion:The results show that the formulation that contain drug: PVP-K30: SLS in ratio 1:0.75:0.25 is the best one and can be utilized to formulate azilsartan medoxomil nanosuspension.

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Section: The Particle Size and Pdi For Different Formulations Of Diffmentioning

confidence: 99%

Formulation and in Vitro Evaluation of Azilsartan Medoxomil Nanosuspension

Jassem

Rajab

2017

Int J Pharm Pharm Sci

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“…9 Através deste processo, nanocristais de diferentes fármacos foram preparados como o cilostazol (estrutura o), que apresentou um aumento na sua biodisponibilidade quando aplicado em cachorros Beagle. 25 Outros exemplos incluem iboprufeno 26 (estrutura p), budesonida 27 (estrutura q), espironolactona 28 (estrutura r), insulina 29 (estrutura s), itraconazol (estrutura e), hidroxi-itraconazol 30 (estrutura t) e Mk-0869 31 (estrutura u).…”

Section: Polimorfismo Nos Nanocristaisunclassified

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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“…Particle size reduction is a very effective way to enhance the solubility. Solubility of smaller particles is higher than bigger ones due to the enhanced surface area [32]. Nanosizing of drug particles has been proven to be a tangible option for achieving enhanced solubility [33].…”

Section: Introductionmentioning

confidence: 99%

Unusual anti-leukemia activity of nanoformulated naproxen and other non-steroidal anti-inflammatory drugs

Kumar

Siril

Javid

2016

Materials Science and Engineering: C

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The non-steroidal anti-inflammatory drugs (NSAIDs) are the most widely used pharmaceuticals worldwide. Interestingly, many of them have significant anticancer properties too. However, the poor water solubility of certain NSAIDs limits their application for cancer treatment. Nanosizing of such drugs can help to improve the solubility and this may result in enhanced anticancer activities too. Moreover, over dosages and the accompanying side effects of NSAIDs can be minimized by improving their solubility and bioavailability. Successful nanoformulation of three NSAIDs: ibuprofen (IBP), ketoprufen (KP) and naproxen (NAP) using a novel evaporation assisted solvent-antisolvent interaction (EASAI) method is reported here. Three water soluble and biocompatible polymers: polyvinylpyrrolidone (PVP), polyvinyl alcohol (PVA) and hydroxypropyl methylcellulose (HPMC) were used to stabilize the drug nanoparticles. Particles having spherical morphology with average size below 30 nm were thoroughly characterized using dynamic light scattering and field emission scanning electron microscopy (FESEM) imaging. The nanoformulation resulted in ten to fifteen fold improvements in the solubility and significant enhancement in the in-vitro drug release profiles of the NSAIDs. Anticancer screening of the nanoformulated NSAIDs against five different cancer cell lines such as MCF-7 (Human breast cancer cell line), (Human pancreatic cancer cell line) MIA-PA-CA-2, (Human colon cancer cell line) HT-29, (Human leukemia cell line) Jurkat and (human ovarian carcinoma cell line) A2780 was performed. All the nanoformulated samples showed improved anticancer activity against the Leukemia cancer cell line, out of which NAP-PVP showed the highest anti-cancer activity. The anti-Leukemia activity of NAP-PVP was more than twice that of doxorubicin which is a standard anticancer drug.

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Preparation and evaluation of nanosuspensions for enhancing the dissolution of poorly soluble drugs

Cited by 336 publications

References 21 publications

Formulation and in Vitro Evaluation of Azilsartan Medoxomil Nanosuspension

Formulation and in Vitro Evaluation of Azilsartan Medoxomil Nanosuspension

Tecnologia de nanocristais em fármacos

Unusual anti-leukemia activity of nanoformulated naproxen and other non-steroidal anti-inflammatory drugs

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