Microemulsion formulation for enhanced absorption of poorly soluble drugs

Kawakami, Kenji; Yoshikawa, Tomohiro; Hayashi, Takashi; Nishihara, Yoko; Masuda, Kazuyoshi

doi:10.1016/s0168-3659(02)00050-0

Cited by 190 publications

(83 citation statements)

References 14 publications

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“…Número de mortes de Artemia salina frente às frações testadas e suas respectivas concentrações com o resultado da CL50% no intervalo de confiança de 95% (Molento 2004). O aumento da biodisponibilidade de fármacos esta correlacionado com a solubilização de substâncias pouco solúveis bem como com a diminuição da dose administrada, garantindo além de vantagens econômicas, a diminuição de efeitos adversos (Kawakami et al 2002). Apesar dos resultados estarem abaixo dos padrões recomendados pela WAAVP (World Association for the Advancement of Veterinary Parasitology), ressalta-se que muitos anti-helmínticos químicos não reduzem os níveis de infecção parasitária, devido à resistência desenvolvida por populações de parasitas (Coles et al 1992).…”

Section: Resultsunclassified

Ação anti-helmíntica do extrato hidroalcóolico da raiz da Tarenaya spinosa (Jacq.) Raf. no controle de Haemonchus contortus em ovinos

et al. 2014

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Pesq. Vet. Bras. 34(10):942-946, outubro 2014 942 RESUMO.-Para investigar o potencial anti-helmíntico do extrato hidroalcóolico da raiz de Tarenaya spinosa, como alternativa no controle do nematóide gastrintestinal Haemonchus contortus de ovinos, foram realizados testes in vitro com Artemia salina, em seguida, sobre coproculturas contendo ovos do helminto, avaliando a ação ovicida e larvicida do extrato. Após os testes preliminares, foi realizado o teste in vivo em 20 ovinos machos os quais foram divididos em quatro tratamentos Grupo 1: ivermectina 1%; Grupo 2: sem tratamento; Grupo 3: extrato hidroalcóolico de T. spinosa 150μg/mL; Grupo 4: extrato hidroalcóolico de T. spinosa 300μg/mL, amostras de fezes e de sangue foram coletadas para exames parasitológicos e hematológicos. No teste in vitro, a toxicidade frente a A. salina foi de 150μg/mL, obteve--se eficiência de 81,53% sobre ovos e larvas do H. contortus. No teste in vivo, a avaliação da eficácia dos tratamentos foi realizada pelo teste de redução na contagem de ovos fecais (RCOF), os grupos tratados com Ivermectina e T. spinosa a 150μg/mL e 300μg/mL obtiveram os melhores resultados, reduzindo o OPG após 28 dias em 40,6, 41 e 40,2% respectivamente, revelando assim seu potencial fitoterápico para fins de controle de nematódeos gastrintestinais em ovinos. To investigate the anthelmintic potential of hydroalcoholic extract of the root of Tarenaya spinosa, as an alternative in the control of gastrointestinal nematode Haemonchus contortus in sheep, in vitro tests were performed with Artemia salina then on stool cultures containing helminth eggs, assessing ovicidal and larvicidal action of the extract. After preliminary tests, the in vivo test was performed in 20 male sheep were divided into four treatments: Group 1 Ivermectin 1 %, Group 2: untreated; Group 3: hydroalcoholic extract of T. spinosa 150μg/ mL; Group 4: hydroalcoholic extract T. spinosa 300μg/mL, stool samples and blood were collected for parasitological and haematological tests. In in vitro tests, toxicity against A. salina was 150μg/mL, there was obtained 81.53% efficiency against eggs and larvae of H. contortus. In vivo test, evaluating the effectiveness of treatments was performed by reduction test in faecal egg count (RCOF), the groups treated with Ivermectin and T. spinosa the 150μg/mL and 300μg/mL obtained the best results, reducing OPG after 28 days in 40.6, 41 and 42.6% respectively, thus revealing its herbal potential for control of gastrointestinal nematodes in sheep.INDEX TERMS: Tarenaya spinosa, Haemonchus contortus, ovicidal and/or larvicidal action.

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Section: Resultsunclassified

Ação anti-helmíntica do extrato hidroalcóolico da raiz da Tarenaya spinosa (Jacq.) Raf. no controle de Haemonchus contortus em ovinos

et al. 2014

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“…The sample taken as the microemulsion phase was confirmed to have a microemulsion size not exceeding 200 nm as reported in a previous study (Gershanik et al, 1998), on the basis of results obtained using a Nano Zeta-Sizer (Table I) (Malvern Instruments, Worcestershire UK). This microemulsion appears to be the most effective mode for the enhanced absorption owing to its physical characteristics, because the formation of microemulsion droplets proceeds very quickly and the droplet size is likely to be the smallest (Kawakami et al, 2002). The effect of the emulsion droplet size on the affinity between the droplets and the intestinal mucosa has been previously investigated by Gershanik et al (1998) who found that the optimal droplet size was in the range of 100-500 nm.…”

Section: Construction Of Pseudo-ternary Phase Diagramsmentioning

confidence: 98%

Preparation and Evaluation of Novel Fenofibrate-loaded Self-Microemulsifying Drug Delivery System (SMEDDS)

2010

Journal of Pharmaceutical Investigation

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− Fenofibrate has been used for many years to lower cholesterol levels and its pharmacokinetic profile is well understood. However, due to its low solubility in water, it has low bioavailability after oral administration. In order to improve the dissolution rate, fenofibrate was formulated into a self-microemulsifying drug delivery systems (SMEDDS). We used pseudo-ternary phase diagrams to evaluate the area of microemulsification, and an in vitro dissolution test was used to investigate the dissolution rate of fenofibrate. The optimized formulation for in vitro dissolution assessment consisted of Lauroglycol FCC (60%), Solutol HS 15 (27%), and Transcutol-P (13%). The mean droplet size of the oil phase in the microemulsion formed from the SMEDDS was about 130 nm. The dissolution rate of fenofibrate from SMEDDS was significantly higher than that of the reference tablet. Our studies suggested that the fenofibrate containing SMEDDS composition can effectively increase the solubility and oral bioavailability of poorly water-soluble drugs.

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“…When the weight ratio of labrasol to plurol oleique ® (Km) was 1:1, the microemulsion area in diagram was the maximum. It has been reported that at the optimum Km value, cosurfactant molecules could exactly insert into the cavities between surfactant molecules (Kawakami et al, 2002).…”

Section: Phase Studymentioning

confidence: 99%

Investigation of microemulsion system for transdermal delivery of ligustrazine phosphate

Cui¹,

Li²,

Gu³

et al. 2011

Afr. J. Pharm. Pharmacol.

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Ligustrazine phosphate is commonly used as an efficient drug to treat a variety of cardiovascular disorders with frequent administration for a short biological half-life. The purpose of the present study was to investigate a microemulsion system for transdermal delivery of ligustrazine phosphate for the convenient, efficient and safe administration. The existence regions of microemulsions containing isopropyl myristate, labrasol, plurol oleique ® and water were investigated in pseudo-ternary phase diagrams, according to which microemulsion vehicles were prepared to observe average diameter, pH value, stability and evaluate respective effect of each component on percutaneous delivery in vitro. The prepared microemulsions had average diameters ranging from 32.1 to 108.7 nm, mild pH values and suitable stability. The optimized microemulsion with permeation flux of 41.01 g/cm 2 /h across rat skin in vitro, showed no obvious irritation on back skin of rabbits. The results indicated that the studied microemulsion system might be a promising vehicle for transdermal delivery of ligustrazine phosphate.

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Microemulsion formulation for enhanced absorption of poorly soluble drugs

Cited by 190 publications

References 14 publications

Ação anti-helmíntica do extrato hidroalcóolico da raiz da Tarenaya spinosa (Jacq.) Raf. no controle de Haemonchus contortus em ovinos

Ação anti-helmíntica do extrato hidroalcóolico da raiz da Tarenaya spinosa (Jacq.) Raf. no controle de Haemonchus contortus em ovinos

Preparation and Evaluation of Novel Fenofibrate-loaded Self-Microemulsifying Drug Delivery System (SMEDDS)

Investigation of microemulsion system for transdermal delivery of ligustrazine phosphate

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