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. 2012 Apr;20(2):161-70.
doi: 10.1016/j.jsps.2011.10.001. Epub 2011 Oct 31.

Ethosomes and ultradeformable liposomes for transdermal delivery of clotrimazole: A comparative assessment

Rahul G S Maheshwari  1 , Rakesh K Tekade, Piyoosh A Sharma, Gajanan Darwhekar, Abhishek Tyagi, Rakesh P Patel, Dinesh K Jain
Affiliations

Ethosomes and ultradeformable liposomes for transdermal delivery of clotrimazole: A comparative assessment

Rahul G S Maheshwari et al. Saudi Pharm J. 2012 Apr.

Abstract

THE OBJECTIVE OF WORK WAS TO FORMULATE, EVALUATE AND COMPARE THE TRANSDERMAL POTENTIAL OF NOVEL VESICULAR NANOCARRIERS: ethosomes and ultradeformable liposomes, containing clotrimazole (CLT), an anti-fungal bioactive. The ethosomal formulation (ET4) and ultradeformable liposomal (UL) formulation (TT3) showed highest entrapment 68.73 ± 1.4% and 55.51 ± 1.7%, optimal nanometric size range 132 ± 9.5 nm and 121 ± 9.7 nm, and smallest polydispersity index 0.027 ± 0.011 and 0.067 ± 0.009, respectively. The formulation ET4 provided enhanced transdermal flux 56.25 ± 5.49 μg/cm(2)/h and decreased the lag time of 0.9 h in comparison to TT3 formulation (50.16 ± 3.84 μg/cm(2)/h; 1.0 h). Skin interaction and FT-IR studies revealed greater penetration enhancing effect of ET4 than TT3 formulation. ET4 formulation also had the highest zone of inhibition (34.6 ± 0.57 mm), in contrast to TT3 formulation (29.6 ± 0.57 mm) and marketed cream formulation (19.0 ± 1.00 mm) against candidal species. Results suggested ethosomes to be the most proficient carrier system for dermal and transdermal delivery of clotrimazole.

Keywords: Anticandidal efficiency; Atomic force microscopy; Ethosomes; Nanocarriers; Ultradeformable liposomes.

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Figures

Figure 1A
Figure 1A
Photomicrograph of ET4 formulation as seen by TEM (transmission electron microscopy).
Figure 1B
Figure 1B
Photomicrograph of TT3 formulation as seen by TEM (transmission electron microscopy).
Figure 2A
Figure 2A
Photomicrographs of ET4 formulation as seen by AFM (atomic force microscopy).
Figure 2B
Figure 2B
Photomicrographs of TT3 formulation as seen by AFM (atomic force microscopy).
Figure 3
Figure 3
FT-IR spectra of rat skin after 8 h. (A) Untreated skin, (B) Hydroethanolic solution, (C) TT3 formulation, (D) ET4 formulation.
Figure 4
Figure 4
Comparative cumulative amount of CLT permeated from ET4 formulation, TT3 Formulation, hydroethanolic solution and plain drug solution in a 24 h study via abdominal rat skin.
Figure 5A
Figure 5A
Model schematic for skin delivery from ethosomal system.
Figure 5B
Figure 5B
Ultradeformable transfersomes compressing through minute pores in the Stratum corneum.
See this image and copyright information in PMC

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