Encapsulation of bio active compound ursolic acid as proniosomes and its evaluation

Munish Garg, Parul Garg

Abstract


In the present study, novel proniosomal gel of ursolic acid was prepared by encapsulation of the drug in a mixture of span 60,
cholesterol and alcohol by coacervation phase separation method to overcome the bioavailability problem of this potential
biologically active compound. The formulated system was characterized for size, drug entrapment, in‑vitro drug release studies and in‑vivo anti‑inflammatory effect through animal model. In‑vitro release data of ursolic acid from proniosomal gel revealed a time dependent near linear relationship. Entrapment efficiency of the formulated gel was found > 90% and total % cumulative release of ursolic acid satisfactory as 60.8% after 24 h. Release pattern was also found almost constant. In‑vivo evaluation revealed that the developed formulation exhibited significant anti‑inflammatory value (P < 0.05) in carrageenan induced rat paw edema model and was found quite comparable with the standard diclofenac gel (voveran gel) in terms of % inhibition of edema.
Key words: Non‑steroidal anti‑inflammatory drugs, proniosomes, topical drug delivery, ursolic acid

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Kim KA, Lee JS, Park HJ, Kim JW, Kim CJ, Shim IS, et al. Inhibition of

cytochrome P450 activities by oleanolic acid and ursolic acid in human

liver microsomes. Life Sci 2004;74:2769‑79.

Baricevic D, Sosa S, Della Loggia R, Tubaro A, Simonovska B, Krasna A,

et al. Topical anti‑inflammatory activity of Salvia officinalis L. leaves: The

relevance of ursolic acid. J Ethnopharmacol 2001;75:125‑32.

Vasconcelos MA, Royo VA, Ferreira DS, Crotti AE, Andrade e Silva ML,

Carvalho JC, et al. In vivo analgesic and anti‑inflammatory activities of

ursolic acid and oleanoic acid from Miconia albicans (Melastomataceae).

Z Naturforsch C 2006;61:477‑82.

Pandey G. Some important anticancer herbs: a review. Int Res J Pharm

;2:45‑52.

Parfent’eva EP. Effect of ursolic acid and its derivatives on lipid

metabolism in experimental atherosclerosis. Chem Abstr 1979;9:9279.

Shai LJ, McGaw LJ, Aderogba MA, Mdee LK, Eloff JN. Four

pentacyclic triterpenoids with antifungal and antibacterial activity

from Curtisia dentata (Burm.f) C.A. Sm. leaves. J Ethnopharmacol

;119:238‑44.

Liu J. Pharmacology of oleanolic acid and ursolic acid. J Ethnopharmacol

;49:57‑68.

Laszczyk MN. Pentacyclic triterpenes of the lupane, oleanane and ursane

group as tools in cancer therapy. Planta Med 2009;75:1549‑60.

Nair B, Taylor‑Gjevre R. A review of topical diclofenac use in

musculoskeleton disease. Pharmaceuticals 2010;3:1892‑908.

Crofford LJ. Use of NSAIDs in treating patients with arthritis. Arthritis

Res Ther 2013;15 Suppl 3:S2.

Li Y, Xing D, Chen Q, Chen WR. Enhancement of chemotherapeutic

agent‑induced apoptosis by inhibition of NF‑kappaB using ursolic acid.

Int J Cancer 2010;127:462‑73.

Huang HC, Huang CY, Lin‑Shiau SY, Lin JK. Ursolic acid inhibits IL‑1beta

or TNF‑alpha‑induced C6 glioma invasion through suppressing the

association ZIP/p62 with PKC‑zeta and downregulating the MMP‑9

expression. Mol Carcinog 2009;48:517‑31.

Khanna D, Sethi G, Ahn KS, Pandey MK, Kunnumakkara AB, Sung B,

et al. Natural products as a gold mine for arthritis treatment. Curr Opin

Pharmacol 2007;7:344‑51.

Ringbom T, Segura L, Noreen Y, Perera P, Bohlin L. Ursolic acid from

Plantago major, a selective inhibitor of cyclooxygenase‑2 catalyzed

prostaglandin biosynthesis. J Nat Prod 1998;61:1212‑5.

Manikrao AM, Khatale PN, Jawarkar RD, Vyas JV, Mahajan DT, Masand VH,

et al. Presuming the probable anti‑inflammatory mechanism of ursolic

acid: A plant derived pentacyclic triterpenoid, using molecular docking.

Scholar Res Libr 2011;1:9‑13.

Blazek‑Welsh AI, Rhodes DG. Maltodextrin‑based proniosomes. AAPS

Pharm Sci 2001;3:E1.

Bairwa NK, Choudhary D. Proniosome: A review. Asian J Biochem Pharm

Res 2011;2:690‑4.

Goyal C, Ahuja M, Sharma SK. Preparation and evaluation of

anti‑inflammatory activity of gugulipid‑loaded proniosomal gel. Acta

Pol Pharm 2011;68:147‑50.

Niemiec SM, Ramachandran C, Weiner N. Influence of nonionic

liposomal composition on topical delivery of peptide drugs into

pilosebaceous units: An in vivo study using the hamster ear model.

Pharm Res 1995;12:1184‑8.

Arunothayanun P, Bernard MS, Craig DQ, Uchegbu IF, Florence AT. The

effect of processing variables on the physical characteristics of non‑ionic

surfactant vesicles (niosomes) formed from a hexadecyl diglycerol ether.

Int J Pharm 2000;201:7‑14.

Vora B, Khopade AJ, Jain NK. Proniosome based transdermal delivery

of levonorgestrel for effective contraception. J Control Release

;54:149‑65.

Fang JY, Yu SY, Wu PC, Huang YB, Tsai YH. In vitro skin permeation of estradiol

from various proniosome formulations. Int J Pharm 2001;215:91‑9.

Hu C, Rhodes DG. Proniosomes: A novel drug carrier preparation. Int

J Pharm 1999;185:23‑35.

Shanmugam MK, Dai X, Kumar AP, Tan BK, Sethi G, Bishayee A. Ursolic acid

in cancer prevention and treatment: Molecular targets, pharmacokinetics

and clinical studies. Biochem Pharmacol 2013;85:1579‑87.

Alam MI, Baboota S, Kohli K, Ali J, Ahuja A. Pharmacodynamic evaluation

of proniosomal transdermal therapeutic gel containing celecoxib. Sci

Asia 2010;36:305‑11.

Alsarra IA, Bosela AA, Ahmed SM, Mahrous GM. Proniosomes as a drug

carrier for transdermal delivery of ketorolac. Eur J Pharm Biopharm

;59:485‑90.

Yoshioka T, Sternberg B, Florence AT. Preparation and properties of

vesicles (niosomes) of sorbitan monoesters (Span 20, 40, 60 and 80)

and a sorbitan triester (Span 85). Int J Pharm 1994;105:1‑6.

Bhaskaran S, Panigarhi L. Formulation and evaluation of niosomes using

different non‑ionic surfactants. Indian J Pharm Sci 2002;64:63‑5.




DOI: http://dx.doi.org/10.22377/ajp.v7i4.337

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