LIPOSOMAL GELS AS CARRIERS FOR SAFER TOPICAL DELIVERY OF TAZAROTENE
Abstract
The aim is to design a liposomal delivery system for topical administration of tazarotene capable of providing controlled and localized release of the encapsulated drug in order to minimize adverse effects associated with its topical use. Tazarotene loaded liposomes were prepared and characterized for entrapment efficiency, particle size and stability. Tazarotene liposomal gels were formulated and evaluated comparatively with commercial gel with respect to primary skin irritation and skin permeation . The effect of vesicular incorporation of tazarotene on its accumulation into hairless rat skin from liposomal suspension and gels were studied. The results of the study showed that the maximum entrapment efficiency recorded (93.49%±0.25) was achieved by formula having 1:1 lipoid S 100 to cholesterol molar ratio. The mean particle size of liposomal formulae ranged from (5.68µm-0.72µm). The stability profile of the selected system assessed for 90 days at refrigerated temperature showed no sign of sedimentation or color change with (86.27% ±0.44) of drug retained. All liposomal suspension and gels revealed higher drug retention compared to commercial gel, lesser skin irritancy and greater skin tolerance was also observed.  Â
References
[2] Guenther LC. Topical tazarotene therapy for psoriasis, acne vulgaris, and photoaging. Skin Therapy Letter. 2002; 7: 1-4.
[3] Chiricozzi A, Chimenti S. Effective topical agents and emerging perspective in the treatment of psoriasis. Expert. Rev. Dermatol. 2012; 7(3): 283-293.
[4] Thielitz A, Gollnick H.Topical retinoids in acne vulgaris. Am.J.Clin.Dermtol.2008; 9(6): 369-381.
[5] Jaratt M, Werner CP, Saenz AB. Tazarotene foam versus tazarotene gel: A randomized relative bioavailability study in acne vulgaris. Clin. Drug Invest. 2013;33 (4): 283-289.
[6] El-Sayed MA, Abdallah OY, Naggar VF, Khalafallah, NM. Lipid vesicles for skin delivery of drugs: Reviewing three decades of research. Int. J. Pharm. 2007; 332 (1-2): 1-16.
[7]El-Maghraby GM, Williams AC, Barry BW. Liposomes and skin: From drug delivery to model membranes. Eur. J. Pharm. Sci. 2008; 34 (4-5): 203-222.
[8] El-Maghraby GM, Williams AC, Barry BW. Can drug-bearing liposomes penetrate intact skin? J. Pharm. Pharmacol.2006; 58 (4): 415-429.
[9] Maestrelli F, González-RodrÃguez ML, Rabasco AM, Mura P. Effect of preparation technique on the properties of liposomes encapsulating ketoprofen–cyclodextrin complexes aimed for transdermal delivery. Int. J. Pharm. 2006; 312 (1-2): 53-60.
[10] El-Samaligy MS, El-Gazayerly ON, Mansour S. Preparation, Freeze drying and stability of chloramphenicol liposomes. Bull. Fac. Pharm. Cairo Univ.2004; 42 :57-68.
[11] Mourtas S, Haikoa M, Theodoropoulou M, Tsakioglou C, Antimisiaris SG. The effect of added liposomes on the rheological properties of a hydrogel: A systematic study. J.Colloids and Interface Sci. 2008; 317(2): 611-619.
[12] Mourtas S, Haikoa M, Theodoropoulou M, Tsakioglou C, Antimisiaris SG. Liposomal drugs dispersed in hydrogels: Effect of liposomes, drug and gel properties on drug release kinetics. J.Colloids and Interface Sci. 2007; 55 (2): 212-221.
[13] P. Mura, L. Celesti, C. Murratzu, S. Corsi, S. Furlanetto, P. Corti, In vitro studies of simulated percutaneous absorption: Influence of artificial membrane impregnation agent, Acta Techn. Leg. Med. 1993; 4 :121–136.
[14] Montenegro L, Panico AM, Ventimiglia A , Bonina FB. In vitro retinoic acid release and skin permeation from different liposome formulations. Int. J. Pharm. 1996; 133: 89- 96.
[15] Qiu Y, Gao Y, Hu K, Li F. Enhancement of skin permeation of docetaxel: A novel approach combining microneedle and elastic liposomes. J. Control Rel. 2008; 129 (2): 144-150.
[16] Manconi M, Sinico C, Valenti D, Lai F, Fadda AM. Niosomes as carriers for tretinoin: III. A study into the in vitro cutaneous delivery of vesicle-incorporated tretinoin. Int. J. Pharm.2006 ; 311 (1-2): 11-19.
[17] Mandawgade SD, Patravale VB. Development of SLNs from natural lipids: Application to topical delivery of tretinoin. Int. J. Pharm. 2008;363 (1-2): 132-138.
[18] Fang Y, Tsai Y, Wu P, Hunag Y. Comparison of 5-aminolevulinic acid-encapsulated liposome versus ethosome for skin delivery for photodynamic therapy. Int. J. Pharm.2008; 356 (1-2):144-152.
[19] Sankhyan A, Pawar P. Recent trends in noisome as vesicular drug delivery system. J. Appl. Pharmaceut. Sci. 2012; 2: 20-32.
[20] Dubeya V, Mishraa D, Duttaa T, Nahara M, Sarafb DK, Jain NK. Dermal and transdermal delivery of an anti-psoriatic agent via ethanolic liposomes. J. Control Rel. 2007; 123 (2): 148-154
[21] Singh, R. Topical liposomal system for localized and controlled drug delivery. J. dermatol. Sci. 1996;13 :107-111.
[22] Mura P, Maestrelli F, González-RodrÃguez ML, Michelacci I, Ghelardini C, Rabasco AM. Development, characterization and in vivo evaluation of benzocaine-loaded liposomes. Eur. J. Pharm. Biopharm. 2007; 67 (1): 86-95.
[23] Hathout RM, Mortada ND , Mansour S, Guinedi AS. Liposomes as an ocular delivery system for acetazolamide: In vitro and in vivo Studies. AAPS Pharm. Sci. Tech. 2007; 8 (1): 1-12.
[24] Hoare TR, Kohane DS. Hydrogels in drug delivery: Progress and challenges. Polymer .2008; 49:1993-2007.
[25] Masini V, Bonte F, Meybeck A, Wepierre J. Cutaneous bioavailability in hairless rats of tretinoin in liposomes or gels. J. Pharm. Sci. 1993; 82: 17–21.
[26] Krajiˇsnikc D , Dragicevic-Curica N , Winterb S, Stuparc M, Milicc J, Gitterd B, Fahra A. Temoporfin-loaded liposomal gels: Viscoelastic properties and skin penetration. Int. J.Pharm.2009; 373: 77-84.
[27] Padamwar MN, PokharkarVB. Development of vitamin loaded topical liposomal formulation using factorial design approach: Drug deposition and stability. Int. J. Pharm. 2006; 320: 37–44.
[28] Contreras MJ, Soriano MM, Dieguez AR. In vitro percutaneous absorption of all-trans retinoic acid applied in free form or encapsulated in stratum corneum lipid liposomes. Int. J. Pharm. 2005; 297: 134–145.
[29]Patil P, Bhowmick M, Pandey GK, Joshi A, Dubey B. Design and evaluation of tazarotene loaded liposome gel for effective treatment of psoriasis and acne. J. Biomed. Pharm. Res. 2013; 2 (6): 19-29.