Effect of abrasion induced by a rotating brush on the skin permeation of solutes with varying physicochemical properties

2008 ◽  
Vol 68 (3) ◽  
pp. 724-734 ◽  
Author(s):  
F AKOMEAH
Author(s):  
Panithi Raknam ◽  
Sirirat Pinsuwan ◽  
Thanaporn Amnuaikit

Phenylethyl Resorcinol (PR) is a cosmeceutical skin lightening agent and the purpose of this study was to enhance its stability by using liposomal cream formulation which increases local efficacy and safety. Liposome formulation was prepared by modified ethanol injection method, and it contained soy phosphatidyl choline (SPC), cholesterol (CHO), Tween 80 (TW80) and deoxycholic acid (DA) mixed with 2% PR. The physicochemical properties, skin permeation as well as cellular study were evaluated in order to obtain the optimized formulation. The optimized liposome formulation composed of SPC:TW80:DA (84:16:2.5) and exhibited vesicle size, polydispersity index (PDI) and zeta potential of 286.4±8.04 nm, 0.317±0.03 and -39.20±3.85 mV, respectively. Entrapment efficiency (EE) of liposome formulation was 93.55±0.05%. The vesicle was spherical in shape and showed good physicochemical stability for 4 months. The skin permeation study demonstrated that liposome with a negative charge could result in a high PR skin deposition value of 1732.76±216.24 µg/cm2 after 24 h. Cellular study showed that liposome formulation could inhibit melanin content in B16 melanoma cells and enhance cell viability in HaCaT keratinocyte cells. The optimized PR liposome was incorporated in cream and investigated physicochemical properties, stability and skin permeation. Liposomal PR cream showed a good stability and a superior result than PR cream in skin permeation parameters, as well as in tyrosinase inhibition.


2014 ◽  
Vol 2014 ◽  
pp. 1-10 ◽  
Author(s):  
Praveen Kumar Gaur ◽  
Shikha Mishra ◽  
Vidhu Aeri

Context. Most new drugs have low water solubility and liposome is an important formulation to administer such drugs; however, it is quite unstable and has negligible systemic absorption.Objective. Aceclofenac nanovesicles were made using guggul lipid for formulating stable transdermal formulation.Materials and Methods. Guggul lipid was formulated into vesicles along with cholesterol and dicetyl phosphate using film hydration method. The formulations were analyzed for physicochemical properties and stability. Then its skin permeation and anti-inflammatory activity were determined.Results. Both categories of vesicles (PC and GL) showed optimum physicochemical properties; however, accelerated stability study showed considerable differences. GL-1 was appreciably stable for over 6 months at 4°C. Corresponding gels (PCG-1 and GLG-1) showedCmaxvalues at 4.98 and 7.32 μg/mL along with theTmaxvalues at 4 and 8 hours, respectively. GLG-1 inhibited edema production by 90.81% in 6 hours.Discussion. PC liposomes are unstable at higher temperature and upon longer storage. The formulation with higher lipid content (GL-1) showed good drug retention after 24 hours and appreciable stability both at higher temperature and for longer duration. Guggul lipid being a planar molecule might be stacked in vesicle wall with cholesterol.Conclusion. The composition of the nanovesicle played an important role in stability and drug permeation. Guggul lipid is suitable for producing stable vesicles.


Pharmaceutics ◽  
2021 ◽  
Vol 13 (9) ◽  
pp. 1457
Author(s):  
Himanshu Kathuria ◽  
Harish K. Handral ◽  
Saera Cha ◽  
Diep T. P. Nguyen ◽  
Junyu Cai ◽  
...  

The study aims to investigate the propylene glycol-based liposomes named ‘proposomes’ in enhancing skin permeation of drugs with different physicochemical properties. Ibuprofen, tofacitinib citrate, rhodamine B, and lidocaine were loaded into proposomes. These drug formulations were analyzed for particle size, zeta potential, polydispersity index, entrapment efficiency, and in vitro skin permeation. The confocal laser scanning microscopy was performed on skin treated with calcein and rhodamine B laden proposomes. The transdermal delivery relative to physicochemical properties of drugs such as logP, melting point, molecular weight, solubility, etc., were analyzed. We tested the safety of the proposomes using reconstructed human skin tissue equivalents, which were fabricated in-house. We also used human cadaver skin samples as a control. The proposomes had an average diameter of 128 to 148 nm. The drug’s entrapment efficiencies were in the range of 42.9–52.7%, translating into the significant enhancement of drug permeation through the skin. The enhancement ratio was 1.4 to 4.0, and linearly correlated to logP, molecular weight, and melting point. Confocal imaging also showed higher skin permeation of calcein and rhodamine B in proposome than in solution. The proposome was found safe for skin application. The enhancement of skin delivery of drugs through proposomes was dependent on the lipophilicity of the drug. The entrapment efficiency was positively correlated with logP of the drug, which led to high drug absorption.


2019 ◽  
Vol 567 ◽  
pp. 118477 ◽  
Author(s):  
Astrid Pany ◽  
Victoria Klang ◽  
Caroline Peinhopf ◽  
Angela Zecevic ◽  
Johanna Ruthofer ◽  
...  

2011 ◽  
Vol 419 (1-2) ◽  
pp. 154-160 ◽  
Author(s):  
Yi-Dong Yan ◽  
Jun Ho Sung ◽  
Dong Won Lee ◽  
Jung Sun Kim ◽  
Eun-Mi Jeon ◽  
...  

2007 ◽  
Vol 30 (11) ◽  
pp. 2211-2216 ◽  
Author(s):  
Krishna Hari Bhandari ◽  
Madhuri Newa ◽  
Sung II Yoon ◽  
Jung Sun Kim ◽  
Ki Young Jang ◽  
...  

2002 ◽  
Vol 91 (1) ◽  
pp. 171-179 ◽  
Author(s):  
Francesco Paolo Bonina ◽  
Maria Grazia Rimoli ◽  
Lucia Avallone ◽  
Francesco Barbato ◽  
Marzia Amato ◽  
...  

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