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. 2014 Feb 6:2014:534210.
doi: 10.1155/2014/534210. eCollection 2014.

Formulation and evaluation of guggul lipid nanovesicles for transdermal delivery of aceclofenac

Praveen Kumar Gaur  1 , Shikha Mishra  2 , Vidhu Aeri  2
Affiliations

Formulation and evaluation of guggul lipid nanovesicles for transdermal delivery of aceclofenac

Praveen Kumar Gaur et al. ScientificWorldJournal. .

Abstract

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) showed C max values at 4.98 and 7.32 μg/mL along with the Tmax values 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.

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Figures

Figure 1
Figure 1
Photomicrograph of PC-1 and GL-1 (×10000) in TEM: (a) PC-1 and (b) GL-1.
Figure 2
Figure 2
In vitro drug release profile of the developed nanovesicle formulations with respect to CPG.
Figure 3
Figure 3
Ex vivo drug permeation of developed nanovesicle gels through human skin with respect to CPG and CF.
Figure 4
Figure 4
Drug deposition profile of developed nanovesicle gels in different layers of skin with respect to CPG and CF; SC: stratum corneum; VED: viable epidermis; D: dermis; RF: receptor fluid.
Figure 5
Figure 5
Plasma drug concentration profile of selected nanovesicle gels with respect to CF.
Figure 6
Figure 6
% edema inhibition provided by selected formulations (GLG-1, PCG-1, CF, and Aceclofenac).
See this image and copyright information in PMC

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