389
Views
20
CrossRef citations to date
0
Altmetric
Research Article

Preparation and characterization of microemulsion formulations of nicotinic acid and its prodrugs for transdermal delivery

, &
Pages 834-843 | Received 21 Jun 2012, Accepted 27 Aug 2012, Published online: 03 Oct 2012

References

  • Said HM, Nabokina SM, Balamurugan K, Mohammed ZM, Urbina C, Kashyap ML. Mechanism of nicotinic acid transport in human liver cells: Experiments with HepG2 cells and primary hepatocytes. Am J Physiol, Cell Physiol 2007;293:C1773–C1778.
  • Durrer A, Walther B, Racciatti A, Boss G, Testa B. Structure-metabolism relationships in the hydrolysis of nicotinate esters by rat liver and brain subcellular fractions. Pharm Res 1991;8:832–839.
  • Grundy SM, Mok HY, Zech L, Berman M. Influence of nicotinic acid on metabolism of cholesterol and triglycerides in man. J Lipid Res 1981;22:24–36.
  • Vaccari CS, Hammoud RA, Nagamia SH, Ramasamy K, Dollar AL, Khan BV. Revisiting niacin: Reviewing the evidence. J Clin Lipidol 2007;1:248–255.
  • Tunaru S, Kero J, Schaub A, Wufka C, Blaukat A, Pfeffer K et al. PUMA-G and HM74 are receptors for nicotinic acid and mediate its anti-lipolytic effect. Nat Med 2003;9:352–355.
  • Drug Information Provided by Lexi-Comp. Niacin The Merck Manuals Online Medical Library 2009.
  • Maccubbin D, Koren MJ, Davidson M, Gavish D, Pasternak RC, Macdonell G et al. Flushing profile of extended-release niacin/laropiprant versus gradually titrated niacin extended-release in patients with dyslipidemia with and without ischemic cardiovascular disease. Am J Cardiol 2009;104:74–81.
  • Jacobson EL, Jacobson MK, Kim H, Kim M, Qasem JG. Topical formulations for the transdermal delivery of niacin and methods of treating hyperlipidemia. US Patent 6677361. 2004.
  • Opinion of the Scientific Committee on Food on the Tolerable Upper Intake Levels of Nicotinic Acid and Nicotinamide (Niacin). Scientific committee on food SCF/ CS/ NUT/ UPPLEV/ 39 Final. 2002:1–20.
  • Kane MP, Hamilton RA, Addesse E, Busch RS, Bakst G. Cholesterol and glycemic effects of Niaspan in patients with type 2 diabetes. Pharmacotherapy 2001;21:1473–1478.
  • Pieper JA. Overview of niacin formulations: Differences in pharmacokinetics, efficacy, and safety. Am J Health Syst Pharm 2003;60:S9–14; quiz S25.
  • Pieper JA. Understanding niacin formulations. Am J Manag Care 2002;8:S308–S314.
  • National Drugs and Poisons Schedule Committee. Record of Reasons of Meeting 53. June 2008;206–207.
  • University of Arizona: Southwest Environmental Health Sciences Center. Available at: http://swehsc.pharmacy.arizona.edu. Accessed on: March 2010.
  • Weiner M. Clinical pharmacology and pharmacokinetics of nicotinic acid. Drug Metab Rev 1979;9:99–106.
  • Jacobson EL, Kim H, Kim M, Wondrak GT, Jacobson MK. (2008). Developing topical prodrugs for skin cancer prevention. In: Alberts DS, Hess LM, eds. Fundamentals of Cancer Prevention. Verlag Berlin Heidelberg: Springer, 215–237.
  • Catz P, Shinn W, Kapetanovic IM, Kim H, Kim M, Jacobson EL et al. Simultaneous determination of myristyl nicotinate, nicotinic acid, and nicotinamide in rabbit plasma by liquid chromatography-tandem mass spectrometry using methyl ethyl ketone as a deproteinization solvent. J Chromatogr B Analyt Technol Biomed Life Sci 2005;829:123–135.
  • Badgett CO, Provost RC, Ogg CL, Woodward CF. Nicotinic acid. Water-insoluble esters and amides. J Am Chem Soc 1945;67:1135–1138.
  • Kogan A, Garti N. Microemulsions as transdermal drug delivery vehicles. Adv Colloid Interface Sci 2006;123-126:369–385.
  • Kaur IP, Kapila M, Agrawal R. Role of novel delivery systems in developing topical antioxidants as therapeutics to combat photoageing. Ageing Res Rev 2007;6:271–288.
  • Heuschkel S, Goebel A, Neubert RH. Microemulsions–modern colloidal carrier for dermal and transdermal drug delivery. J Pharm Sci 2008;97:603–631.
  • Pappinen S, Urtti A. (2006). Microemulsions in topical drug delivery. In: Smith EW, Maibach HI, eds. Percutaneous Penetration Enhancers. 2nd edition. Boca Raton: CRC Press, Taylor & Francis Group, 109–116.
  • Djordjevic L, Primorac M, Stupar M. In vitro release of diclofenac diethylamine from caprylocaproyl macrogolglycerides based microemulsions. Int J Pharm 2005;296:73–79.
  • Peira E, Carlotti ME, Trotta C, Cavalli R, Trotta M. Positively charged microemulsions for topical application. Int J Pharm 2008;346:119–123.
  • Kristl J, Volk B, Gasperlin M, Sentjurc M, Jurkovic P. Effect of colloidal carriers on ascorbyl palmitate stability. Eur J Pharm Sci 2003;19:181–189.
  • Kreilgaard M. Influence of microemulsions on cutaneous drug delivery. Adv Drug Deliv Rev 2002;54 Suppl 1:S77–S98.
  • Djekic L, Primorac M. The influence of cosurfactants and oils on the formation of pharmaceutical microemulsions based on PEG-8 caprylic/capric glycerides. Int J Pharm 2008;352:231–239.
  • Walters KA, Brain KR. (2002). Dermatological formulation and transdermal systems. In: Walters KA, ed. Dermatological and Transdermal Formulations. New York: Marcel Dekker Inc, 349–432.
  • Teichmann A, Heuschkel S, Jacobi U, Presse G, Neubert RH, Sterry W et al. Comparison of stratum corneum penetration and localization of a lipophilic model drug applied in an o/w microemulsion and an amphiphilic cream. Eur J Pharm Biopharm 2007;67:699–706.
  • Yuan Y, Li SM, Mo FK, Zhong DF. Investigation of microemulsion system for transdermal delivery of meloxicam. Int J Pharm 2006;321:117–123.
  • Subramanian N, Ghosal SK, Acharya A, Moulik SP. Formulation and physicochemical characterization of microemulsion system using isopropyl myristate, medium-chain glyceride, polysorbate 80 and water. Chem Pharm Bull 2005;53:1530–1535.
  • Fanun M. A study of the properties of mixed nonionic surfactants microemulsions by NMR, SAXS, viscosity and conductivity. J Mol Liq 2008;142:103–110.
  • Kim BY, Doh HJ, Le TN, Cho WJ, Yong CS, Choi HG et al. Ketorolac amide prodrugs for transdermal delivery: Stability and in vitro rat skin permeation studies. Int J Pharm 2005;293:193–202.
  • Müller B, Kasper M, Surber C, Imanidis G. Permeation, metabolism and site of action concentration of nicotinic acid derivatives in human skin. Correlation with topical pharmacological effect. Eur J Pharm Sci 2003;20:181–195.
  • Abraham MH, Acree WE Jr. Characterisation of the water-isopropyl myristate system. Int J Pharm 2005;294:121–128.
  • Stinchcomb AL, Paliwal A, Dua R, Imoto H, Woodard RW, Flynn GL. Permeation of buprenorphine and its 3-alkyl-ester prodrugs through human skin. Pharm Res 1996;13:1519–1523.
  • Sinha VR, Kaur MP. Permeation enhancers for transdermal drug delivery. Drug Dev Ind Pharm 2000;26:1131–1140.
  • Pathan IB, Setty CM. Chemical penetration enhancers for transdermal drug delivery systems. Trop J Pharmaceut Res 2009;8:173–179.
  • Santos P, Watkinson AC, Hadgraft J, Lane ME. Application of microemulsions in dermal and transdermal drug delivery. Skin Pharmacol Physiol 2008;21:246–259.
  • Davis AF, Gyuric RJ, Hadgraft J, Pellet MA, Walters KA. (2002). Formulation strategies for modulating skin permeation. In: Walters KA, ed. Dermatological and Transdermal Formulations. New York: Marcel Dekker Inc, 271–318.
  • Williams AC, Barry BW. Penetration enhancers. Adv Drug Deliv Rev 2004;56:603–618.
  • Funke AP, Schiller R, Motzkus HW, Günther C, Müller RH, Lipp R. Transdermal delivery of highly lipophilic drugs: In vitro fluxes of antiestrogens, permeation enhancers, and solvents from liquid formulations. Pharm Res 2002;19:661–668.

Reprints and Corporate Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

To request a reprint or corporate permissions for this article, please click on the relevant link below:

Academic Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

Obtain permissions instantly via Rightslink by clicking on the button below:

If you are unable to obtain permissions via Rightslink, please complete and submit this Permissions form. For more information, please visit our Permissions help page.