Transdermal delivery of zidovudine: effect of terpenes and their mechanism of action

Narishetty, Sunil T.; Panchagnula, Ramesh

doi:10.1016/j.jconrel.2003.11.022

Cited by 191 publications

(93 citation statements)

References 35 publications

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“…However, the main barrier to drug permeation through any of these membranes is the stratum corneum (SC) that has been reported to differ in terms of lipid composition, water content and morphological characteristics (thickness, number of pores and follicles). To overcome this barrier to transdermal delivery, formulation scientists have investigated a number of techniques such as chemical enhancement [2]- [4], microemulsions [5]- [8], nanoemulsions [9]- [11], cosolvent systems [12]- [14], ethosomes [15] [16] and organic solvents [17] [18]. Gabapentin, 2-[1-(aminomethyl) cyclohexyl] acetic acid is an excitatory amino acid antagonist.…”

Section: Introductionmentioning

confidence: 99%

Transdermal Delivery of Gabapentin: Effect of Cosolvent and Microemulsion on Permeation through the Rat Skin

Mbah¹,

Nnadi²

2014

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The objective of the present study was to examine the influence of cosolvent system and microemulsion formulation on in-vitro skin permeation of gabapentin, furthermore, to characterize the physicochemical properties of drug-loaded oil-in-water (o/w) and water-in-oil (w/o) cremophor 40-based microemulsions in comparison to the blank counterparts. The cosolvent system prepared by homogenous mixing is composed of ethanol-water and propylene glycol-water mixture (90:10, 80:20, 70:30 v/v) respectively. The microemulsion consisted of coconut oil, water and mixture of cremophor 40 (surfactant) and ethanol (cosurfactant) and was prepared by aqueous phase titration method. Physicochemical properties of microemulsions were determined using reported procedures. Transdermal flux for gabapentin was studied in-vitro using modified Franz diffusion cells. The physicochemical properties of drug-loaded microemulsions and their blank counterparts were generally alike, however, slight variation in pH and viscosity was observed probably due to the intrinsic properties of the drug. The ethanol-water system (70:30 v/v) gave higher flux for gabapentin when compared to propylene glycol-water system (70:30 v/v). The w/o microemulsion formulations resulted in, higher flux for gabapentin when compared to o/w formulations. FTIR spectra of the untreated stratum corneum, when compared to cosolvent system and microemulsion treated stratum corneum, suggest the mechanism of permeation to be disruption of lipid bilayers and keratin denaturation of the stratum corneum. The results show that incorporation of gabapentin into microemulsions did not change the microemulsion type. The in vitro permeation data obtained from experimental work suggest that the cosolvent system (ethanol-water 70:30 v/v) and w/o microemulsion formulations respectively, can be successfully used as potential vehicles in developing transdermal therapeutic systems for gabapentin.

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Section: Introductionmentioning

confidence: 99%

Transdermal Delivery of Gabapentin: Effect of Cosolvent and Microemulsion on Permeation through the Rat Skin

Mbah¹,

Nnadi²

2014

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“…The saturation solubilities of model drugs with and without Z. bungeanum oil or three terpene compounds were thus measured to investigate the effect of these enhancers on thermodynamic activities of model drugs (Narishetty and Panchagnula, 2004). As evident from Table 3, Z. bungeanum oil could significantly increase the saturation solubilities of OT, TMP, FA, and PR (P<0.05), while it did not obviously alter the saturation solubility of GP in comparison to the control (P>0.05).…”

Section: Possible Action Mechanismsmentioning

confidence: 99%

Essential oil from Zanthoxylum bungeanum Maxim. and its main components used as transdermal penetration enhancers: a comparative study

Chen

et al. 2014

J. Zhejiang Univ. Sci. B

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Lan et al. / J Zhejiang Univ-Sci B (Biomed & Biotechnol) Abstract:Our previous studies had confirmed that the essential oil from Zanthoxylum bungeanum Maxim. (Z. bungeanum oil) could effectively enhance the percutaneous permeation of drug molecules as a natural transdermal penetration enhancer. The aim of the present study is to investigate and compare the skin penetration enhancement effect of Z. bungeanum oil and its main components on traditional Chinese medicine (TCM) active components. Toxicities of Z. bungeanum oil and three selected terpene compounds (terpinen-4-ol, 1,8-cineole, and limonene) in epidermal keratinocytes (HaCaT) and dermal fibroblast (CCC-ESF-1) cell lines were measured using an MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) assay. Five model drugs in TCM external preparations, namely osthole (OT), tetramethylpyrazine (TMP), ferulic acid (FA), puerarin (PR), and geniposide (GP), which were selected based on their lipophilicity denoted by logKo/w, were tested using in vitro permeation studies in which vertical Franz diffusion cells and rat abdominal skin were employed. The secondary structure changes of skin stratum corneum (SC) and drug thermodynamic activities were investigated to understand their mechanisms of action using Fourier transform infrared (FTIR) spectroscopy and saturation solubility studies, respectively. It was found that Z. bungeanum oil showed lower toxicities in both HaCaT cells and CCC-ESF-1 cells compared with three terpene compounds used alone. The enhancement permeation capacities by all tested agents were in the following increasing order: terpinen-4-ol≈1,8-cineole

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“…On the day of experiment, skin was brought to room temperature, epidermal sheet was cleaned by washing with distilled water and dried under vacuum and examined for cuts or holes if any. Then skin samples were mounted over the diffusion cells in such a way that SC side faced the donor compartment whereas the dermis faced the receiver compartment (Narishetty & Panchagnula, 2004).…”

Section: Selection Of Animal Modelmentioning

confidence: 99%

Nanoethosomes mediated transdermal delivery of vinpocetine for management of Alzheimer’s disease

et al. 2014

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Aim: To develop and statistically optimize nanoethosomal formulation for transdermal delivery of vinpocetine as an anti-Alzheimer's drug. Materials and methods: Box-Behnken experimental design was applied for optimization of nanoethosomes. The independent variables were phospholipid (X 1 ), Tween 80 (X 2 ) and Ethanol (X 3 ) while entrapment efficiency (Y 1 ), particle sizes (Y 2 ), elasticity (Y 3 ) and flux (Y 4 ) were the dependent variables. Results and conclusion: Optimized nanoethosomal vinpocetine formulation with mean particle size 50.57 AE 26.11 nm showed 97.51 AE 0.86% entrapment efficiency, achieved mean transdermal flux 925.60 AE 39.80 mg/cm 2 /h and elasticity of 86.61 AE 2.88. Ex-vivo study of nanoethosomal formulation showed a significant increase flux and entrapment efficiency compared with control vinpocetine solution. Our results suggest that nanoethosome is an efficient carrier for transdermal delivery of vinpocetine as compared to its oral form.

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Transdermal delivery of zidovudine: effect of terpenes and their mechanism of action

Cited by 191 publications

References 35 publications

Transdermal Delivery of Gabapentin: Effect of Cosolvent and Microemulsion on Permeation through the Rat Skin

Transdermal Delivery of Gabapentin: Effect of Cosolvent and Microemulsion on Permeation through the Rat Skin

Essential oil from Zanthoxylum bungeanum Maxim. and its main components used as transdermal penetration enhancers: a comparative study

Nanoethosomes mediated transdermal delivery of vinpocetine for management of Alzheimer’s disease

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