Solubilization of Ester-Type Permeation Enhancers Using a Non-ionic Surfactant Derived from Castor Oil with Various Co-surfactants

In this study, we investigated the effect of different permeation enhancers at different concentrations viz. oleic acid, olive oil and castor oil from transdermal gel for transdermal delivery of venlafaxine, a newer antidepressant. It is a first line drug in the treatment of depression and inhibits brain serotonin and norepinephrine neuronal reuptake. It is also used in the treatment of anxiety disorders. Transdermal delivery of venlafaxine hydrochloride may result in enhanced patient compliance by reducing the incidence of the undesirable GI problems associated with its multiple oral dosing. The differential scanning colorimetry study was used to investigate the drug-polymer interaction. The prepared gels were evaluated for several physico-chemical parameters such as drug content, spreadability, pH, viscosity and physical appearance to justify their suitability for topical use. The in vitro permeation studies were performed by using Franz diffusion cell and rat skin as a semi permeable membrane. This indicate that penetration enhancers in 5% v/w concentration enhance the permeation of venlafaxine hydrochloride but oleic acid show maximum permeation rate was 197 µg/cm2/hr as compared to olive oil (154.69µg/cm2/hr) and castor oil (175.8µg/cm2/hr). It is further optimized by increasing the concentration of permeation enhancer at levels as high as 10% v/w and 15% v/w. The result indicates that increase in the concentration of enhancer enhances the percutaneous permeation of venlafaxine. Oleic acid was found to be superior to olive oil and castor oil implying the ability of oleic acid to increase the drug diffusion by SC lipid disruption and increase partition coefficient into SC. The permeation rate of venlafaxine hydrochloride with 15% v/w oleic acid was higher (rat abdominal skin flux = 8.507 µg/cm2/h) than with 15% v/w olive oil and castor oil. These studies show promising potential of transdermal patches of venlafaxine.

Download Full-text

Influence of the oleic phase and co-surfactant addition in non-ionic microemulsified systems

Research Society and Development ◽

10.33448/rsd-v10i2.12902 ◽

2021 ◽

Vol 10 (2) ◽

pp. e58410212902

Author(s):

Fabiola Dias da Silva Curbelo ◽

Alfredo Ismael Curbelo Garnica ◽

Beatriz Sales Cavalcanti Nascimento ◽

Giovanna Lais Rodrigues Leal ◽

Tarsila Melo Tertuliano ◽

...

Keyword(s):

Thermogravimetric Analysis ◽

Phase Diagrams ◽

Castor Oil ◽

Isopropyl Alcohol ◽

Ionic Surfactant ◽

Experimental Conditions ◽

Ternary Diagrams ◽

Pine Oil ◽

Type Iv ◽

The Ideal

Microemulsion is a thermodynamically stable dispersion consisting of an aqueous and an organic phases, both stabilized by surfactant molecules and when in need, co-active surfactant. The nature and structure of these components are essential in the formulation of microemulsified systems. For this, the construction of phase diagrams can be a fundamental tool to characterize the ideal experimental conditions for the existence and operation of microemulsions. Thus, the present work had as objective to obtain a comparison between microemulsions with different compositions through the construction of ternary diagrams, aiming to achieve the most stable system. To produce microemulsified systems, a non-ionic surfactant (Ultranex NP 60), a co-surfactant (Isopropyl Alcohol), two organic phases (pine oil and castor oil) and an aqueous phase (glycerin solution) were used. Also complementing the study, rheological tests of the oleic phases were accomplished, as well as their thermogravimetric analysis. The focus of the reached ternary diagrams was to find the system with the largest Winsor type IV region (microemulsion). It was verified this region had a significant increase by the addition of the co-surfactant in the medium and using a vegetable oil, such as pine oil, since it promotes strong surfactant-oil interactions on the interface.

Download Full-text

FORMULATION, OPTIMIZATION AND EVALUATION OF MATRIX TYPE TRANSDERMAL DRUG DELIVERY SYSTEM OF ANTIEMETIC DRUG USING ESSENTIAL OILS AND NON-IONIC SURFACTANT AS PERMEATION ENHANCERS

INDIAN DRUGS ◽

10.53879/id.55.07.10833 ◽

2018 ◽

Vol 55 (07) ◽

pp. 77-78

Author(s):

N Madkaikar ◽

A Shirodker ◽

S Bhangle ◽

R. Gude

Keyword(s):

Essential Oils ◽

Moisture Absorption ◽

Transmission Rate ◽

Moisture Loss ◽

Tween 20 ◽

Ionic Surfactant ◽

Permeation Enhancers ◽

Matrix Type ◽

Ondansetron Hydrochloride ◽

Percent Moisture

This study involved developing a matrix-type transdermal therapeutic system comprising of ondansetron hydrochloride with 7:3 ratio of hydrophilic and hydrophobic polymeric combinations using solvent evaporation technique. The effects of permeation enhancers were studied at the concentrations of 2.5% and 5% using essential oils such as menthol oil, eucalyptus oil, clove oil, lemon grass oil and the blend of best volatile oil with Tween 20 dibutyl phthalate and glycerin were used as plasticizers. Formulated patches were evaluated for thickness, folding endurance, drug content, percent moisture absorption, percent moisture loss, tensile strength and water vapour transmission rate. There was no physicalchemical incompatibility between the drug and the polymers. The results of in vitro drug release studies showed that the blend of menthol oil and Tween 20 exhibited maximum release. The optimized formulation was found to be stable during the stability studies. The developed transdermal patches increase the efficacy and improve the bioavailability.

Download Full-text