Microemulsion for Intradermal Delivery Of Cetyl Alcohol and Octyl Dimethyl PABA

Linn, Edwards E.; Pohland, Raymond C.; Byrd, Tiffany

doi:10.3109/03639049009114917

Cited by 30 publications

(14 citation statements)

References 3 publications

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“…For instance, oral microemulsion formulations were successfully developed for cyclosporine, a highly lipophilic and poorly aqueous soluble drug, to improve its oral bioavailability and reduce the absorption variations (Ritschel et al, 1990;Kim et al, 1996). Microemulsions are also considered for topical (Linn, 1990;Garcia-Celma et al, 1994), transdermal (Thevenin et al, 1996), and parenteral (von Corswant et al, 1998) drug delivery systems. For instance, the nasal absorption of diazepam from ethyl laurate (15%)/Tween 80:propylene glycol (PG):ethanol (EA) at a 1:1:1 weight ratio (70%)/water (15%) microemulsion was fairly rapid at a dose of 2 mg/kg.…”

Section: Research Articlementioning

confidence: 98%

Rapid-onset sildenafil nasal spray carried by microemulsion systems:in vitroevaluation andin vivopharmacokinetic studies in rabbits

Chen

Sheu

et al. 2011

Xenobiotica

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An oleic acid-based microemulsion system with a member of the Tween series or Cremophor EL as the surfactant and a short-chain alcohol as the cosolvent was developed for rapid-onset intranasal delivery of sildenafil. The phase behaviour and solubilization capacity of the microemulsion system were characterized, and nasal absorption of sildenafil from the microemulsion formulations was investigated in rabbits. Sildenafil displayed a high solubility of 124 mg/mL in the microemulsion consisting of 40% oleic acid, 10% H(2)O, and 50% Tween 80:ethanol (EA) (at a 1:4 weight ratio). Nasal absorption of sildenafil from this microemulsion was found to be fairly rapid. With a 10-mg dose, the onset of action was arrived instantly following intranasal administration and the duration was over 3 h using an in vivo rabbit studies. In addition, nasal ciliotoxicity studies were carried out using in vivo rat nasal mucosa model and showed no ciliotoxicity. Therefore, the prepared systems are no serious nasal ciliotoxicity for intranasal administration. The microemulsion system composed of oleic acid, Tween 80, EA, and water may be a practical approach for the rapid-onset delivery of sildenafil for the treatment of erectile dysfunction.

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Section: Research Articlementioning

confidence: 98%

Rapid-onset sildenafil nasal spray carried by microemulsion systems:in vitroevaluation andin vivopharmacokinetic studies in rabbits

Chen

Sheu

et al. 2011

Xenobiotica

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“…Nesse estudo utilizou-se a célula de Frans e micrótono criostático de micro-seccionamento para quantificar a velocidade e a profundidade da penetração das substâncias, respectivamente 56 . A penetração do álcool cetílico contido em ME foi cerca de 3,7 vezes maior que num creme e 5 vezes maior que numa loção correspondente, ao longo de 4 h.…”

Section: Microemulsão De Liberação Transdérmicaunclassified

Microemulsões: estrutura e aplicações como sistema de liberação de fármacos

Oliveira¹,

Scarpa²,

Corrêa³

et al. 2004

Quím. Nova

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Recebido em 25/9/02; aceito em 27/6/03 MICROEMULSIONS: STRUCTURE AND APPLICATION AS DRUG DELIVERY SYSTEMS. Depending on formula composition, microemulsions may be used as a vehicle for drug administration. In this work the main applicable parameters used in the development of pharmaceutical microemulsions (ME) are analyzed. The conceptual description of the system, theoretical parameters related to formation of internal phases and some aspects of ME stability are described. The pseudo ternary phase diagram is used to characterize ME boundaries and to describe different structures in several regions of the diagram. Some applications of ME as drug delivery systems for different administration routes are also analyzed. ME offer advantages as drug delivery systems, because they favor drug absorption, being in most cases faster and more efficient than other methods in delivering the same amount of drug.Keywords: microemulsions; drug incorporation; drug delivery. INTRODUÇÃOA interação de fármacos com interfaces de agregados supramoleculares de compostos anfifílicos ou de polímeros representa um aspecto importante em tecnologia farmacêutica, pelas implicações biológicas da presença destes compostos em fórmulas farmacêuticas, interferindo no perfil de biodisponibilidade, alterando constantes de ionização de fármacos cujo efeito terapêutico depende substancialmente da fração ionizada da droga ou modificando a estabilidade de grande número de compostos de uso terapêutico 1-3 . Independentemente de como se possa definir uma interface, podemos imaginar uma superfície, a partir da qual pode ser descrita uma região externa, contínua, representada pelo meio dispersante, geralmente de natureza aquosa, e outra região, representada pela pró-pria interface, com características particulares e propriedades físico-químicas bastante diferentes das do meio dispersante.Estas propriedades diferenciadas permitem a utilização destas estruturas em tecnologia farmacêutica, com o objetivo de ampliar as alternativas de aplicação em terapêuticas específicas 4 . Assim, uma membrana biológica, a superfície de um polímero, micelas, microemulsões e lipossomas representam exemplos de interfaces, em cuja superfície uma série de fenômenos especiais pode ocorrer.Raramente a experiência clínica com agentes terapêuticos satisfaz as expectativas criadas em torno de resultados pré-clínicos com medicamentos, desde que entre o local de administração e o órgão ou tecido alvo existe uma série de barreiras anatômicas, químicas ou biológicas que contrariam a obtenção do efeito terapêutico desejado. Neste contexto está inserido o conceito dos sistemas transportadores de fármacos, os quais são capazes de compartimentalizar a substância ativa e direcioná-la para os sítios onde deverá exercer o efeito farmacológico, além de poder controlar a velocidade de liberação, sem alterar a estrutura química da molécula transportada [4][5][6] . Dessa forma, esses sistemas envolvem as seguintes concepções bási-cas: a-sistemas matriciais ou monolíticos, nos quais o fármaco está ...

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“…[3][4][5][6] However, very few studies report the use of emulsions as possible vehicles for nasal delivery. Kararli et al have proved an enhanced bioavailability of a poorly soluble, modified tripeptide renin inhibitor from a nasal emulsion as against an oral emulsion.…”

Section: Introductionmentioning

confidence: 99%

Development and Evaluation of Nitrendipine Nanoemulsion for Intranasal Delivery

Jain

Patravale²

2009

Journal of Biomedical Nanotechnology

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The clinical efficacy of Nitrendipine (NDP), a potent antihypertensive molecule, is limited due to its low oral bioavailability (10% to 20%) resulting from its extensive first-pass metabolism. The purpose of the present investigation was to enhance the bioavailability of NDP through formulating a nanoemulsion for its intranasal delivery. A Caproyl 90 ® based nanoemulsion sytem with Tween 80 as the surfactant, Transcutol P ® and Solutol HS-15 ® as solubiliser and cosurfactant respectively, was developed. A single isotropic region, which is considered as a bicontinuous nanoemulsion, was identified in the pseudo-ternary phase diagrams developed at various Tween 80: Transcutol P ® : Solutol HS-15 ® ratios. NDP was solubilized in a system consisting of Tween 80: Transcutol P ® : Solutol HS-15 ® at 1:2:1 weight ratio. The developed nanoemulsion was safe for nasal administration as confirmed by nasal histopathlogy studies with the mean globule size of 98.50 nm. The drug content per actuation was found to be 99 58 ± 0 05%, with no significant changes over a period of one month. In vivo absorption studies revealed that NDP absorption from the nanoemulsion had a rapid onset of action and a relative bioavailability of 60.44%, significantly greater than the marketed oral tablets.

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Microemulsion for Intradermal Delivery Of Cetyl Alcohol and Octyl Dimethyl PABA

Cited by 30 publications

References 3 publications

Rapid-onset sildenafil nasal spray carried by microemulsion systems:in vitroevaluation andin vivopharmacokinetic studies in rabbits

Rapid-onset sildenafil nasal spray carried by microemulsion systems:in vitroevaluation andin vivopharmacokinetic studies in rabbits

Microemulsões: estrutura e aplicações como sistema de liberação de fármacos

Development and Evaluation of Nitrendipine Nanoemulsion for Intranasal Delivery

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