Percutaneous absorption enhancers: mechanisms and potential

Rodrigues, Letícia Norma Carpentieri; Zanluchi, Juliana Modolo; Grebogi, Ivanna Hinke

doi:10.1590/s1516-89132007000700006

Cited by 22 publications

(14 citation statements)

References 52 publications

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“…Propylene glycol acts as a penetration enhancer for the drugs which are better soluble in alcohol than in water. The solvation of keratin within the stratum corneum by competition with water for the hydrogen bond binding sites and the intercalation in the polar head groups of the lipid bilayers by propylene glycol are postulated as mechanisms of action for the penetration enhancement [27]. The synergistic combinatorial effect of ethanol and soya lecithin is depicted to be responsible for a deeper drug loaded distribution and penetration into the skin layers [28].…”

Section: Preparation and Evaluation Of Ethosomal Gelmentioning

confidence: 99%

Development, Characterization and Transdermal Delivery of Dapsone and an Antibiotic Entrapped in Ethanolic Liposomal Gel for the Treatment of Lapromatous Leprosy

Tiwari¹,

Tiwari²,

Wal³

et al. 2018

TONMJ

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Background and Objective: Applying Ethosomal Gels (EGs) in transdermal drug delivery systems has evoked considerable interest because of their good water-solubility and biocompatibility. The aim of present study was to prepare and characterize ethosomes of antileprotic drug Dapsone (DAP) together with an antibiotic Cloxacillin Sodium (CLXS) which may deliver these drugs to targeted site more efficiently than marketed gel preparation of DAP and also overcome the problems related with oral administration of CLXS. Methodology: Ethosomes were prepared by cold method then characterized for particle size, Entrapment Efficiency (EE), zeta potential and permeation studies. Vesicular size was determined by Scanning Electron Microscopy (SEM) and found to be varied from 127±9.01 to 215±7.23 nm depending on the concentrations of soya lecithin and ethanol. Results: The average percent drug entrapment efficiency of formulations ranged between 52.31% to 73.51% and 49.07% to 71.91% for DAP and CLXS respectively. The high ethanol concentration in ethosomes has shifted the vesicular charge from positive to negative. It was observed that F1 and F2 formulations were having zeta potential of -25.08±1.03 mV and -50.11±1.97 mV respectively and do not aggregate rapidly. The drug release of ethosomes ranged from 84.68% to 96.58% and 64.89% to 84.21% for DAP and CLXS respectively. Ethosomal gel was prepared with optimized ethosome and studied for its release and physicochemical characteristics. Conclusion: Finally, G5 demonstrated better (p < 0.05) antileprotic effect to improve effectiveness, stability and to reduce side effects and toxicity associated with the chosen drugs in order to treat Leprosy.

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Section: Preparation and Evaluation Of Ethosomal Gelmentioning

confidence: 99%

Development, Characterization and Transdermal Delivery of Dapsone and an Antibiotic Entrapped in Ethanolic Liposomal Gel for the Treatment of Lapromatous Leprosy

Tiwari¹,

Tiwari²,

Wal³

et al. 2018

TONMJ

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“…33 On the other hand, oleic acid is likely to dissolve the ligation of the horny layer by diminishing the lipid-binding temperature. 33,34…”

Section: Discussionmentioning

confidence: 99%

Enhancement of Dermal Delivery of Finasteride Using MicroemulsionSystems

Soleymani

Salimi

2019

Adv Pharm Bull

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Purpose: Finasteride is a pharmaceutical agent that treats hair loss and acne with hormonal patterns. Due to its poor water solubility, and the smaller surface area in comparison to total skin surface area, penetration of the drug into hair follicles and skin is low. The aim of this research was to formulate, characterize and evaluate in vitro skin permeability of finasteride microemulsions (MEs). Methods: Finasteride MEs were prepared using a pseudo-ternary phase diagram method with an appropriate ratio of oil mixture, surfactant-co-surfactant mixture and water. MEs containing 1% finasteride were prepared with a suitable amount of oily phase and surfactant and cosurfactant. The physicochemical properties of these MEs and in vitro skin permeability of MEs were evaluated. Results: The results showed that the mean droplet size range of ME samples was 5–17 nm and pH was 5.1–5.7. The viscosity of MEs ranged from 86.4–209.6 cps. The drug release profile showed that 49.510% of the drug was released (ME-F-6) over the 24 hours of the experiment. The kinetics of drug release from all selected MEs were approximately described by Higuchi and first-order modeling. All ME formulations with different compositions and properties significantly increased flux and permeability coefficient from rat skin. The selected MEs exhibit 99.9% finasteride after six months of storage. Conclusion: This study showed that any change in the content and composition of MEs could change the physical and chemical properties in addition to ME permeability parameters. The MEs increased permeability of the skin to finasteride.

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“…Sifat fisik-kimia obat dipengaruhi oleh koefisien partisi, ukuran molekul, kelarutan, titik leleh, kemampuan ionisasi, serta koefisien difusi. Selain itu, kemampuan pentrasi ke dalam kulit juga dipengaruhi oleh sistem penghantaran obatnya, seperti karakteristik perilisan, komposisi sistem penghantaran obat, serta kemampuan permeasi transdermal [4], [5]. Secara umum permeasi transdermal dapat ditingkatkan melalui 3 mekanisme, yaitu merusak atau mengubah sifat fisik-kimia stratum korneum, interaksi dengan interselular dalam stratum korneum, serta meningkatkan partisi obat dalam stratum korneum [6].…”

Section: Gambar 2 Rute Penetrasi Obat Transdermal [4]unclassified

“…Sedangkan pada elektroosmosis, molekul netral ditranspor dengan aliran pelarut. Aplikasi secara elektroosmosis atau reverse-iontoforesis telah digunakan pada alat GlucoWatch untuk mengukur kadar glukosa darah dari cairan interstisial [1], [4], [5].…”

Section: Iontoforesisunclassified

Review Artikel: Metode untuk Meningkatkan Absorpsi Obat Transdermal

Annisa¹

2020

J. Islamic Pharm.

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The route of administration of transdermal drugs is preferred because it is easy to use. However, there are limitations associated with the difficulty of drugs penetrating into the skin. This is caused by the presence of the stratum corneum which is the main barrier for drug entry into the skin. Penetration of the drug into the skin can be through the trans-epidermal (transcellular and paracellular) route and the trans-appendegeal route depending on the dosage form. To increase the penetration ability of transdermal drugs, it can use chemical enhancers and physical enhancers. Chemical enhancers can be classified based on chemical structure or based on the mechanism of action. Chemical compounds that have the same functional groups can have different mechanisms of action depending on the physical-chemical nature. Chemical enhancers are categorized based on their chemical structure, including: water, alcohol, amides, esters, alcohol ethers, pyrrolidone, hydrocarbons, sulfides, surfactants, terpenes, phospholipids, vesicles. Whereas physical enhancers in the form of drug delivery use external energy to encourage or physically damage the stratum corneum. Physical enhancer methods such as Iontophoresis,

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Percutaneous absorption enhancers: mechanisms and potential

Cited by 22 publications

References 52 publications

Development, Characterization and Transdermal Delivery of Dapsone and an Antibiotic Entrapped in Ethanolic Liposomal Gel for the Treatment of Lapromatous Leprosy

Development, Characterization and Transdermal Delivery of Dapsone and an Antibiotic Entrapped in Ethanolic Liposomal Gel for the Treatment of Lapromatous Leprosy

Enhancement of Dermal Delivery of Finasteride Using MicroemulsionSystems

Review Artikel: Metode untuk Meningkatkan Absorpsi Obat Transdermal

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