The effect of pH and organic ester penetration enhancers on skin permeation kinetics of terbutaline sulfate from pseudolatex-type transdermal delivery systems through mouse and human cadaver skins

Panigrahi, Lalatendu; Pattnaik, Snigdha; Ghosal, Shreya

doi:10.1208/pt060225

Cited by 41 publications

(28 citation statements)

References 17 publications

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“…It is always very important to assess the stability of novel formulations. Stability could be viewed from the degradation of the active ingredients or physical property of the formulation (Panigrahi et al, 2005;Umeyor et al, 2012). In order to determine the change in drug content on storage, stability study was carried out.…”

Section: Bioevaluation Of Transdemal Patchesmentioning

confidence: 99%

Bioactivity of gentamicin contained in novel transdermal drug delivery systems (TDDS) formulated with biodegradable polyesters

Nnamani¹

2013

Afr. J. Pharm. Pharmacol.

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Topical administration of gentamicin, a hydrophilic aminoglycoside antibiotic, is limited by membrane impermeability and toxicity concerns. The purpose of this study was to develop and evaluate the antimicrobial activities of an alternative non-invasive, convenient and cost-effective transdermal drug delivery system (TDDS) containing gentamicin in biodegradable polyester-based matrices. The patches were formulated by solvent evaporation technique using PURASORB ® polymers and evaluated for thermal properties, drug content, physicochemical performance, stability, skin irritation on rat skin and antimicrobial activities against five micro-organisms: Staphylococcus aureus, Escherichia coli, Salmonella typhi, Pseudomonas aeruginosa, and Klebsiella pneumoniae. The differential scanning calorimetry (DSC) results indicated compatibilty between the drug and the polymers. In addition, the formulations showed good drug encapsulation, stability, physicochemical properties, tolerability on rabbit skin and higher zones of inhibition compared with a commercially available gentamicin sulphate cream against S. aureus, E. coli, S. typhi and P. aeruginosa, while K. pneumoniae was mildly susceptible. Compared with the rest of the formulations, patches of PURASORB ® PL 32 exhibited the best stability, tolerability on rat skin and bioactivity. This study has shown that transdermal patches of PURASORB ® PL 32 represent an alternative delivery system for gentamicin for treatment of infections caused by gentamicin-susceptible micro-organisms.

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Section: Bioevaluation Of Transdemal Patchesmentioning

confidence: 99%

Bioactivity of gentamicin contained in novel transdermal drug delivery systems (TDDS) formulated with biodegradable polyesters

Nnamani¹

2013

Afr. J. Pharm. Pharmacol.

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“…To calculate the permeation parameters of the Fick's law equation a graph of penetrated amounts vs. time was plotted. It is possible to calculate the steadystate flux (J) from the slope of the linear portion (2-6 hours) of the graph [24,25]. 8] with high viscosity (589.1 Pas).…”

Section: Permeability Studymentioning

confidence: 99%

Film forming gel for treatment of oral mucositis: In vitro studies.

Attia¹,

Badawy²

2010

Int J Drug delivery

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Oral mucositis is one of the main complications of non-surgical cancer treatments. The present work focuses on the treatment or reduction of oral mucositis by using combined mechanism by formation of physical barrier by forming a film to cover the oral ulcer and use of therapeutic agents, such as diclofenac sodium and ofloxacin separately or in combination. The selected polymers for film forming gel formulations are Hydroxypropylcellulose (HPC), hydroxypropyl methylcellulose (HPMC), sodium carboxymethylcellulose (Na CMC) and carbopol 940 (CP). The residence time in simulated buccal saliva was between 5.5 to 6 hours for all formulations. The in-vitro release data of the investigated drugs from the prepared formulations followed zero-order and diffusion mechanism. The permeability studies data revealed that diclofenac sodium showed higher permeability from Na CMC/CP (2:0.3%) than from HPMC 4%, while in case of ofloxacin higher permeability was shown from Na CMC/CP (2:0.3%) than from HPMC/HPC (2:3%). The permeation parameters for diclofenac sodium and ofloxacin in their combination do not depend on either viscosity or pH, they depend on the type of polymers used.

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“…1,24,25 Já o K p foi calculado a partir do J no steady-state versus a concentração de DDA no compartimento doador (C doador ) conforme Equação 1 sugerida por Ozguney et al.…”

Section: Cálculo Do Fluxo (J) E Do Coeficiente De Permeabilidade (K Punclassified

Estudo de liberação e permeação in vitro do diclofenaco de dietilamônio em microemulsão gel-like

Silva¹,

Santana²,

Bedor³

et al. 2009

Quím. Nova

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Recebido em 25/3/08; aceito em 25/2/09; publicado na web em 3/7/09 IN VITRO RELEASE AND PERMEATION OF A DICLOFENAC DIETHYLAMINE FROM MICROEMULSION GEL-LIKE.The goal of this study was to produce and characterize a new microemulsion gel-like carrier system (MEG) by using the pseudoternary phase-diagram concept. The diclofenac diethylamine (DDA) was incorporated in the MEG and its in vitro release and permeation profiles were performed using Franz-type diffusion cells. The results revealed that the commercial DDA emulgel provided significantly higher K p of DDA (2.2-fold) as compared to the MEG. Similar data were obtained in the permeation studies in which DDA K p 4.7-fold higher. Therefore, MEG presents higher potential as a topical delivery system for DDA when compared to the commercial DDA emulgel.Keywords: diclofenac diethylamine; in vitro release; microemulsion gel-like. INTRODUÇÃOA administração tópica é conhecida como via alternativa da administração oral de ativos medicamentosos e oferece muitas vantagens como a ausência de efeito de primeira passagem, o fato de ser indolor e a facilidade de aplicação. 1 Todavia, uma eficácia tópica só é obtida a partir de fármacos potentes com adequado grau de penetração na pele. 2 Isto tem levado a um crescente interesse pela utilização de promotores de permeação em formulações tópicas, assim como o uso de sistemas de liberação de fármacos com esta capacidade promotora de permeação. 3 As microemulsões (ME) são dispersões isotrópicas, transparentes, termodinamicamente estáveis, usualmente formadas por misturas de quatro componentes, água, óleo, tensoativo e cotensoativo. Apresentam grande potencial como sistemas de liberação e de direcionamento de fármacos, pelas propriedades de solubilizar fármacos hidrofílicos em meio lipofílico, lipofílicos em meio aquoso e anfifílicos na interface óleo/água. 4-10 Além disso, estes sistemas apresentam capacidade de se formarem espontaneamente, podendo existir sob várias formas estruturais (globular a/o e o/a, bicontínuas, cúbicas ou lamelares), 11,12 e atuam como promotores de permeação de vários fármacos, devido ao reduzido tamanho das gotículas formadas, assim como ao seu alto conteúdo de tensoativo, que desorganiza os lipídeos da pele. 5 O diclofenaco de dietilamônio (DDA) é um anti-inflamatório não esteroidal (AINEs) capaz de formar micelas e cristais líquidos liotrópicos em água. 13 Apresenta a capacidade de interagir com os fosfolipídeos da pele, contribuindo para aumentar a fluidez do mesmo no estrato córneo, fazendo com que os lipídios passem de uma forma cristalina ordenada para uma forma líquida desordenada, aumentando, portanto, a permeabilidade cutânea. 5,7 Além disso, o DDA apresenta metabolismo hepático, tempo de meia-vida curto, 14 não sofre metabolismo na pele, não induz tolerância e tem bom coeficiente de partição. 15 Com base nas colocações acima e na importância do tema, o objetivo do presente trabalho foi a obtenção e a caracterização de uma ME, na forma gel (MEG) contendo DDA, como sistema promotor de permeação do f...

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The effect of pH and organic ester penetration enhancers on skin permeation kinetics of terbutaline sulfate from pseudolatex-type transdermal delivery systems through mouse and human cadaver skins

Cited by 41 publications

References 17 publications

Bioactivity of gentamicin contained in novel transdermal drug delivery systems (TDDS) formulated with biodegradable polyesters

Bioactivity of gentamicin contained in novel transdermal drug delivery systems (TDDS) formulated with biodegradable polyesters

Film forming gel for treatment of oral mucositis: In vitro studies.

Estudo de liberação e permeação in vitro do diclofenaco de dietilamônio em microemulsão gel-like

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