Preparation and Characterization of Cyanocobalamin (Vit B12) Microemulsion Properties and Structure for Topical and Transdermal Application

Document Type : Original Article

Authors

Nanotechnology Research Center, Ahvaz Jundishapur University of Medical Sciences, Ahvaz, Iran 2 School of Pharmacy, Ahvaz Jundishapur University of Medical Sciences, Ahvaz, Iran

Abstract

 




Objective(s): The objective of this study was to design a topical microemulsion of Vit B12
and to study the correlation between internal structure and physicochemical properties of the microemulsions. Microemulsions are thermodynamically stable mixtures of water, oil, surfactants and usually cosurfactants with several advantages for topical and transdermal drug delivery. The formulation of microemulsions for pharmaceutical use requires a clear understanding of the properties and microstructures of the microemulsions.
 
Materials and Methods:
In this study, phase behavior and microstructure of traditional and novel microemulsions of Vit B12 have been investigated by Small-angle X-ray (SAXS), differential scanning calorimetery (DSC) and measuring density, particle size, conductivity and surface tension.
Results:
WO and bicontinuous microemulsion with different microstructures were found in novel and traditional formulations. In this study, amount of water, surfactant concentration, oil/ surfactant ratio and physicochemical properties of cosurfactants influenced the microstructures. In both formulations, water behavior was affected by the concentration of the surfactant. Water Solubilization capacity and enthalpy of exothermic peak of interfacial and free water of traditional formulations were more than novel ones. This means that the affinity of water to interfacial film is dependent on the surfactant properties.
Conclusion:
This study showed that both microemulsions provided good solubility of Vit B12 with a wide range of internal structure. Low water solubilization capacity is a common property of microemulsions that can affect drug release and permeability through the skin. Based on Vit B12 properties, specially, intermediate oil and water solubility, better drug partitioning into the skin may be obtained by traditional formulations with wide range of structure and high amount of free and bounded water.

Keywords

References

1. Bagwe RP, Kanicky JR, Palla BJ, Patanjali PK, Shah DO. Improved drug delivery using microemulsion: rationale, recent progress, and new horizons. Crit Rev Ther Drug 2001; 18: 77-140.
2. Tosmic M, Podlogar F, Gasperlin M, Bester-Rogac M, Jamink A. Water- tween 40/imwitor 308-isopropyl myristate microemulsions as delivery systems for ketoprofen: Small-angle X-ray scattering study. Int J Pharm 2006; 327: 170-177.
3. Heuschkel S, Goebel A, Neubert RH. Microemulsion – modern colloidal carrier for dermal and transdermal drug delivery. J Pharm Sci 2008; 97: 603-631.
4. Kreilgaard M. Influence of microemulsions on cutaneous drug delivery. Adv Drug Del Rev 2002; 54: 77-98
5. Boonme P, Krauel K, Graf A, Rades T, Junyaprasert VB. Characterization of microemulsion structure in the pseudoternary phase diagrame of isopropyl palmitate/water/brij 97: 1-butanol. AAPS PharmSciTech 2006; 7: E1-E7
6. Naoui W, Bolzinger MA, Fenet B, Pelletier J, Valoer JP, et al. Microemulsion microstructure influences the skin delivery of an hydrophilic drug. Pharm Res 2011; 28: 1683-1695.
7. Langevin D. Microemulsion- interfacial aspects. Adv Colloid Inter Sci 1991; 34: 583-95.
8. Shinoda K, Kunieda H, Arati T, Saijo H. Principles of attending very large Solubilization: inclusive understanding of the Solubilization of oil and water in aqueous and hydrocarbon media. J Phys Chem 1984; 88: 5126-5129.
9. Zvonar A, Rozman B, Rogac MB, Gasperlin M. The influence of microstructure on celecoxib release from a pharmaceutically applicable system: Mygliol 812/Labrasol /Plurol Oleique /Water mixtures. Acta Chim Slov 2009; 56: 131-138.
10.Podlogar F, Gasperline M, Tomsic M, Jamnik A, Rogac MB. Structural characterisation of water-tween40/ imwitor 308- isopropyl myristate microemulsion using different experimental methods. Int J Pharm 2004; 276: 115-128.
11. Stucker M, Pieck C, Stoerb C, Niedner R, Hartung J, Altemeyer P. Topical Vit B
12 – a new therapeutic approach in atopic dermatitis- evaluation of efficacy and tolerability in a randomized placebo – controlled multicenter clinical trial. Br J Dermatol 2004; 150: 977-983.
12. Stankler L. the Vit B
12 level in psoriatic skin and serum. Br J Dermatol 1969; 81: 911-918.
13. Sharif Makhmal Zadeh B, Moghimi HR, Santos P, Hadgraft J, Lane ME, Rahim F. Formulation of microemulsion systems for improvement of nitrofurazone permeation through silicon membrane as burn wound imitating coverage. Int J Pharmacol 2010; 6(3): 264-270.
14. Acharya A, Sanyal K, Moulik SP. Formulation and characterization of a pharmaceutically useful microemulsion derived from isopropyl myristate, polyoxyethylene (4) lauryl ether (Brij-30), isopropyl alcohol and water. Cur Sci 2001; 881(4):362-370.
15. Bajpai M, Sharma PK, Mittal A. A study of oleic acid oily base for tropical delivery of dexamethasone microemulsion formulations. Asian J Pharm 2009; 208-214.
16. Borhade V, Nair H, Hedge D. Design and evaluated of self-microemulsion drug delivery system of tacrolimus. AAPS PharmSciTech 2008; 9 (1): 13-21.
17. Kim S, Ng WK, Shen S, Dong Y, Tan RBH. Phase behavior, microstructure transition and antiradical activity of sucrose laurate/ PG/ the essential oil of melaleuca alternifolia/ water microemulsion. Colloid & Surf A 2009; 348: 289-297.
18. Eicke HF. The microemulsion concept in nonpolar surfactant solutions. In: Robb ID (ed). Mikroemulsions. Plenum, New York, 1982, p .17-32.
19. Strey R. Microemulsion microstructure and interfacial curvature. Colloid Polym Sci 1994; 272: 10-15.
20. Chen SH, Chang SL, Strey R. Structural evaluation within one-phase region of a three-component microemulsion: water- n-decane-sodium- bis- ethylhexyl sulfosuccinate (AOT). J Chem Phys 1990; 97: 1907-1918.
21.Herrera JR, Peralta RD, Lopez`RG, Cesteros LC, Mendizabal E, Puig JE. Cosurfactant effects on the polymerization of vinyl acetate in anionic media. Polymer 2003; 44: 1795-1802.
22.Bumajdad A, Eastoe J. Conductivity of water-in-oil microemulsions stabilized by mixed surfactants. J Colloid & Interface Sci 2004; 274: 268-276.
23.Garti N, Aserin A, Tiunova I, Funun M. A DSC study of water behavior in wate- in – oil microemulsions stabilized by sucrose esters and butanol. Colloids & Surface 2000; 120: 1-18.
24. Raman IA, Suhaimi H, Tiddy GJ. Liquid crystals and microemulsions formed by mixtures of a non-ionic surfactant with palm oil and its derivatives. Adv Colloid Interface Sci 2003; 106: 109-127.
25. Perez-Casas S, Castillo R, Costas M. Effect of alcohols in AOT reverse micelles. A heat capacity and light scattering study. J Phys Chemo B 1997; 101: 7043–7054.

Files

Share

How to cite

Statistics