scholarly journals EFFECT OF HYDROPHILIC AND HYDROPHOBIC POLYMER MATRIX ON THE TRANSDERMAL DRUG DELIVERY OF ETHINYLESTRADIOL AND MEDROXYPROGESTERONE ACETATE

2019 ◽  
Vol 11 (1) ◽  
pp. 210
Author(s):  
Shikha Baghel Chauhan ◽  
Tanveer Naved ◽  
Nayyar Parvez
Keyword(s):  
Medroxyprogesterone Acetate ◽  
Ethyl Cellulose ◽  
Skin Permeation ◽  
Eudragit Rs ◽  
Hydrophobic Polymer ◽  
In Vitro Permeation ◽  
In Vitro Skin Permeation ◽  
Permeation Studies ◽  
Eudragit Rl

Objective: The aims of the present study were to develop different matrix patches with various ratios of hydrophilic and hydrophobic polymer combinations such as ethyl cellulose (EC) and polyvinylpyrrolidone (PVP) and eudragit RL 100 (ERL) and eudragit RS 100 (ERS) containing ethinylestradiol and medroxyprogesterone acetate and to perform physicochemical characterization and in vitro permeation studies through rat skin.Methods: Six formulations (F1 to F6) were developed by varying the concentration of both hydrophilic and hydrophobic polymer and keeping the drug load constant. Physical parameters and drug excipient interaction studies were evaluated in all the formulations. In vitro, skin permeation profiles of ethinylestradiol and medroxyprogesterone acetate from various formulations were simultaneously characterized in a thermostatically controlled modified Franz Diffusion cell. The physicochemical compatibility of the drug and the polymers was studied by differential scanning calorimetry.Results: The results suggested no physicochemical incompatibility between the drug and the polymers. In vitro permeation studies were performed by using Franz diffusion cells, patches coded as F3 (ethyl cellulose: polyvinylpyrrolidone, 7.5:2.5) and F6 (eudragit RL 100 (ERL) and eudragit RS 100 (ERS), 8:2) can be chosen for further in vivo studies. The results followed Higuchi kinetics (r = 0.9953-0.9979), and the mechanism of release was diffusion mediated. Based on physicochemical and in vitro skin permeation studies of 85.64% (for F3) and 88.62% (for F6) of ethinylestradiol and medroxyprogesterone acetate.Conclusion: The developed transdermal patches are stable, non-irritating and had increased efficacy of ethinylestradiol and medroxyprogesterone acetate and therefore had a good potential for antifertility treatment.

scholarly journals Lipid-based nanocarriers to enhance skin permeation and antioxidant activity of Centella asiatica extract

2018 ◽  
Vol 192 ◽  
pp. 01016
Author(s):  
Boonnada Pamornpathomkul ◽  
Worranan Rangsimawong ◽  
Theerasak Rojanarata ◽  
Praneet Opanasopit ◽  
Chuleerath Chaiyodsilp ◽  
...  
Keyword(s):  
Antioxidant Activity ◽  
Skin Permeation ◽  
Centella Asiatica ◽  
Entrapment Efficiency ◽  
Dpph Assay ◽  
Significant Difference ◽  
In Vitro Skin Permeation ◽  
Permeation Studies ◽  
Solution Formulation

The purpose of this study was to evaluate the use of different formulations, including solution, gel, liposome and niosome for in vitro skin permeation and antioxidant activity of Centella asiatica (CA) extract. The liposomes and niosomes loaded with CA were characterized to observe the physicochemical properties i.e., particle size, zeta potential, percentage of entrapment efficiency (%EE) and percentage of loading efficiency (%LE). In vitro skin permeation studies revealed that liposome formulations had a superior enhancing effect on skin permeation compared to niosome, gel and solution formulation. Upon applied niosome formulations for the delivery of CA extract at 24 hours (h), the antioxidant activity was higher than liposome, gel and solution formulation, as evidenced by the increased in percent inhibition using 2,2-diphenyl-1-picrylhydrazyl (DPPH) assay. However, there was no significant difference in antioxidant activity between niosome and liposome formulations. Accordingly, both the liposome and noisome formulations are promising approaches for transdermal delivery of CA extract for promoting successful antioxidant activity.

scholarly journals Elastic liposomes mediated transdermal delivery of verapamil hydrochloride

2018 ◽  
Vol 8 (6) ◽  
pp. 16-21
Author(s):  
NEHA JAIN ◽  
Ameeta Argal ◽  
Girendra Gautam
Keyword(s):  
Transdermal Delivery ◽  
Skin Permeation ◽  
Entrapment Efficiency ◽  
Sprague Dawley ◽  
Rat Skin ◽  
Verapamil Hydrochloride ◽  
In Vitro Skin Permeation ◽  
Permeation Studies ◽  
Elastic Vesicles

The aim of present investigation was to formulate and characterize elastic liposomes as a delivery system for transdermal delivery of Verapamil hydrochloride, a drug having low oral bioavailability (approx 20%), short biological half-life and extensive first pass metabolism.Verapamil hydrochloride loaded elastic vesicles were prepared by a slightly modified extrusion method using soya phosphatidylcholine and span 80(edge activator). Prepared elastic vesicles were characterized for various parameters such as vesicle shape, vesicle size and size distribution, entrapment efficiency, elasticity measurements, stability studies and in vitro skin permeation studies through excised rat skin (Sprague Dawley) using a locally fabricated Franz diffusion cell. The entrapment efficiency of elastic vesicles was found to be 59.3±3.6%. In vitro skin permeation of verapamil hydrochloride through excised rat skin (Sprague Dawley) revealed that elastic vesicles led to an enhanced transdermal flux (50.2±4.52 mg/cm2/h) of verapamil hydrochloride as compared to liposomes (11.6±2.12mg/cm2/h). Decreased lag time (0.9 h) was also observed in case of elastic liposomes. Our results indicate the feasibility of elastic liposomes for transdermal delivery of verapamil hydrochloride for improved skin permeation. Keywords: Transdermal delivery, Elastic liposomes, Verapamil hydrochloride.  

scholarly journals Development and Evaluation of Ethyl Cellulose-Based Transdermal Films of Furosemide for Improved In Vitro Skin Permeation

2009 ◽  
Vol 10 (2) ◽  
pp. 437-442 ◽  
Author(s):  
Dhaval P. Patel ◽  
Chitral Mallikarjuna Setty ◽  
Gaurav N. Mistry ◽  
Santnu L. Patel ◽  
Tarun J. Patel ◽  
...  
Keyword(s):  
Ethyl Cellulose ◽  
Skin Permeation ◽  
In Vitro Skin Permeation

scholarly journals Use of Curcuma longa in cosmetics: extraction of curcuminoid pigments, development of formulations, and in vitro skin permeation studies

2014 ◽  
Vol 50 (4) ◽  
pp. 885-893 ◽  
Author(s):  
Gisele Mara Silva Gonçalves ◽  
Gustavo Henrique da Silva ◽  
Pedro Paulo Barros ◽  
Silvana Mariana Srebernich ◽  
Cecilia Toyoko Cavalcanti Shiraishi ◽  
...  
Keyword(s):  
Curcuma Longa ◽  
Skin Permeation ◽  
Cell System ◽  
Skin Permeability ◽  
Topical Formulations ◽  
In Vitro Skin Permeation ◽  
Permeation Studies ◽  
Anti Inflammatory ◽  
The Stability

Curcuma longais a ginger family aromatic herb (Zingiberaceae) whose rhizomes contain curcuminoid pigments, including curcumin, a compound known for its anti-inflammatory effects. The objective of this study was to obtain curcuminoid-rich extracts, develop topical formulations thereof, and assess the stability and skin permeation of these formulations. Curcuma longa extracts were obtained and used to develop formulations. Skin permeation studies were conducted in a modified Franz diffusion cell system, and skin retention of curcuminoid pigments was quantified in pig ear membrane. Prepared urea-containing gel-cream formulations were unstable, whereas all others had satisfactory stability and pseudoplastic rheological behavior. The amount of curcuminoid pigments recovered from the receptor solution was negligible. The skin concentration of curcuminoid pigments retained was positive (>20 µg/g of skin, mostly in the stratum corneum), considering the low skin permeability of curcumin. We conclude that development of topical formulations containing curcumin or Curcuma longaextract is feasible, as long as adjuvants are added to improve preservation and durability. The formulations developed in this study enabled penetration of curcumin limited to the superficial layers of the skin and then possibly without a risk of systemic action, thus permitting local use as a topical anti-inflammatory.

Evaluation of a polysiloxane-collagen biphasic membrane: a model for in vitro skin permeation studies

2009 ◽  
Vol 19 (4) ◽  
pp. 289-294 ◽  
Author(s):  
M. Shumilov ◽  
E. Touitou ◽  
B. Godin ◽  
D. Ainbinder ◽  
I. Yosha ◽  
...  
Keyword(s):  
Skin Permeation ◽  
In Vitro Skin Permeation ◽  
Permeation Studies

scholarly journals Design of in vitro skin permeation studies according to the EMA guideline on quality of transdermal patches

2018 ◽  
Vol 125 ◽  
pp. 86-92 ◽  
Author(s):  
Francesco Cilurzo ◽  
Umberto M. Musazzi ◽  
Silvia Franzé ◽  
Guido Fedele ◽  
Paola Minghetti
Keyword(s):  
Skin Permeation ◽  
Transdermal Patches ◽  
In Vitro Skin Permeation ◽  
Permeation Studies

In Vitro Skin Permeation Methodology for Over-The-Counter Topical Dermatologic Products

2019 ◽  
pp. 216847901987533 ◽  
Author(s):  
Luke Oh ◽  
Sojeong Yi ◽  
Da Zhang ◽  
Soo Hyeon Shin ◽  
Edward Bashaw
Keyword(s):  
Product Life Cycle ◽  
Skin Permeation ◽  
Systemic Exposure ◽  
Skin Permeability ◽  
Over The Counter ◽  
In Vitro Permeation ◽  
In Vitro Skin Permeation ◽  
Study Sites

For topically applied over-the-counter (OTC) products, the association of unwanted systemic exposure and adverse events may be difficult to ascertain without a recognition or determination of in vivo absorption. Evaluation of skin permeability using a validated in vitro permeation methodology can provide important information for both initial formulation selection and reformulation during the product life cycle. Additionally, a comparison of permeation rates between formulations using a validated methodology could reduce the number of nonclinical studies needed as part of reformulation. However, many in vitro permeation tests (IVPTs) have produced results with high variability and low reproducibility between study sites. It is unclear if this is due to a lack of a standardized protocol, or lack of control of multiple key experimental factors including skin source, preparation, receptor fluid, and study design. This review presents the authors perspective on the potential regulatory utility of IVPT and proposes steps to improve the accuracy and reproducibility of IVPT. The focus of this review is on topical dermatologic drugs with an initial emphasis on the OTC marketplace where reformulations are more common.

Sign in / Sign up

Export Citation Format

Share Document