Microemulsion formulations for the transdermal delivery of testosterone

Hathout, Rania M.; Woodman, Timothy J.; Mansour, Samar; Mortada, Nahed D.; Geneidi, Ahmed S.; Guy, Richard H.

doi:10.1016/j.ejps.2010.03.008

Cited by 152 publications

(97 citation statements)

References 56 publications

(58 reference statements)

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“…Colloidal formulations have also been shown to enhance transdermal skin penetration. [54][55][56] Results presented here demonstrate that delivery of macromolecules can be effectively achieved without the use of any specific delivery devices or the need to design complex formulations.…”

Section: Discussionmentioning

confidence: 98%

Transdermal Protein Delivery Using Choline and Geranate (CAGE) Deep Eutectic Solvent

Banerjee

Ibsen

Iwao

et al. 2017

Adv Healthcare Materials

163

155

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Transdermal delivery of peptides and other biological macromolecules is limited due to skin's inherent low permeability. Here, the authors report the use of a deep eutectic solvent, choline and geranate (CAGE), to enhance topical delivery of proteins such as bovine serum albumin (BSA, molecular weight: ≈66 kDa), ovalbumin (OVA, molecular weight: ≈45 kDa) and insulin (INS, molecular weight: 5.8 kDa). CAGE enhances permeation of BSA, OVA, and insulin into porcine skin ex vivo, penetrating deep into the epidermis and dermis. Studies using tritium-labeled BSA and fluorescein isothiocyanate labeled insulin show significantly enhanced delivery of proteins into and across porcine skin, penetrating the skin in a time-dependent manner. Fourier transform IR spectra of porcine stratum corneum (SC) samples before and after incubation in CAGE show a reduction in peak area attributed to SC lipid content, suggesting lipid extraction from the SC. Circular dichroism confirms that CAGE does not affect insulin's secondary conformation. In vivo studies in rats show that topical application of 10 U insulin dispersed in CAGE (25 U kg −1 insulin dose) leads to a highly significant 40% drop in blood glucose levels in 4 h that is relatively sustained for 12 h. Taken together, these studies demonstrate that CAGE is a promising vehicle for transdermal delivery of therapeutic proteins; specifically, as a noninvasive delivery alternative to injectable insulin for the treatment of diabetes.

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Section: Discussionmentioning

confidence: 98%

Transdermal Protein Delivery Using Choline and Geranate (CAGE) Deep Eutectic Solvent

Banerjee

Ibsen

Iwao

et al. 2017

Adv Healthcare Materials

163

155

View full text Add to dashboard Cite

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“…The use of microemulsions as a carrier vehicle in the topical formulations of drugs has been shown to improve the permeability of such formulations (Dantas et al, 2010;Hathout, Woodman, Mansour, 2010;Jadhav, Shetye, Kadam, 2010;Rogerio Dora, Andrade, 2010;Tsai et al, 2010). Bolzinger et al (2008) showed that microemulsions based on caffeine have better permeation than pharmaceutical forms, such as emulsion and gel.…”

Section: Anti-inflammatory Activitymentioning

confidence: 99%

Microemulsion based on Pterodon emarginatus oil and its anti-inflammatory potential

Pascoa

Diniz

Florentino

et al. 2015

Braz. J. Pharm. Sci.

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This article reports the development of a pharmaceutical product containing vegetable actives from a Brazilian medicinal plant. The possibility of forming a microemulsion using Pterodon emarginatus ("sucupira") oil was evaluated and the anti-inflammatory potential of this microemulsion was also examined. A formulation was developed using P. emarginatus oil, a mixture of ethoxylated Castor Oil (Ultramone ® R-540/propylene glycol 2:1) (surfactant/cosurfactant) and distilled water at a ratio of 10:15:75, respectively. The microemulsion which was selected was then subjected to the preliminary stability test and analyzed in terms of average diameter of droplets, pH, zeta potential, and polydispersity index, on the 1 st , 7 th , 15 th , and 30 th days after preparation and stored at different temperatures (5 ± 2 °C, 25 ± 2 °C, and 40 ± 2 °C). The anti-inflammatory in vivo activity of both oil and formulation were evaluated, using the experimental model of croton oil-induced ear edema. The preliminary stability test showed that the microemulsion stored at 5 and 25 °C retained its original features throughout the 30-day period. The anti-inflammatory potential of both oil and formulation was shown to be statistically significant (p < 0.001), when compared to the control group, however, the microemulsion proved to be more effective (p < 0.05) than the oil when applied directly to the ear. Descrevemos o desenvolvimento de um produto farmacêutico contendo ativo vegetal baseado em uma planta medicinal brasileira. Foi avaliada a habilidade de formação de uma microemulsão à base do óleo de Pterodon emarginatus (sucupira) e seu potential anti-inflamatório. Uma formulação foi desenvolvida utilizando o óleo de P. emarginatus, mistura de óleo de mamona etoxilado (Ultramona ® R-540)/propilenoglicol (2:1) (tensoativo/cotensoativo) e água destilada, na proporção de 10:15:75, respectivamente. A microemulsão selecionada foi submetida ao teste preliminar de estabilidade e foi analisada quanto ao diâmetro médio das gotículas, pH, potential zeta e índice de polidispersão, no 1º, 7º, 15º e 30º dias após o preparo e foram estocadas em diferentes temperaturas (5±2 °C, 25±2 °C e 40±2 °C). Avaliaram-se a atividade anti-inflamatória in vivo do óleo de sucupira e da formulação, usando o modelo experimental do edema de orelha induzido pelo óleo de cróton. No teste preliminar de estabilidade observou-se que a formulação estocada a 5 °C e a 25 °C mantiveram suas características originais durante 30 dias. O potencial anti-inflamatório de ambos, óleo de sucupira e formulação foi estatisticamente significativo (p <0.001), quando comparado ao controle, porém a microemulsão foi mais eficiente (p <0.05) que o óleo aplicado diretamente nas orelhas dos animais. Unitermos:Pterodon emarginatus/pharmacognosy. Pterodon emarginatus/óleo/atividade antiinflamatória. Plantas medicinais. Microemulsão. Fitoterápico. Tecnologia farmacêutica.

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“…Sodium naproxen (Escobar-Chavez et al, 2005); Sodium diclofenac (Escribano et al, 2003); Lidocaine (Cazares-Delgadillo et al, 2005); Testosterone (Hathout et al, 2010); Mometasone furoate (Senyiğit et al, 2009); Ketorolac (Amrish et al, 2009). …”

Section: Azone ®mentioning

confidence: 99%