Concentration dependency in nicotine skin penetration flux from aqueous solutions reflects vehicle induced changes in nicotine stratum corneum retention

Pharmaceutical Research

Volumn 31, Issue 6, 2014, Pages 1501-1511

  Kuswahyuning, Rina ^a,b   Roberts, Michael S ^a,c  

^a UNIVERSITY OF SOUTH AUSTRALIA   (Australia)

^b GADJAH MADA UNIVERSITY   (Indonesia)

^c UNIVERSITY OF QUEENSLAND   (Australia)

Author keywords

nicotine thermodynamic activity; skin penetration flux; solute concentration; stratum corneum hydration; stratum corneum retention

Indexed keywords

NICOTINE; DRUG VEHICLE; NICOTINIC AGENT; SOLUTION AND SOLUBILITY;

AQUEOUS SOLUTION; ARTICLE; CONCENTRATION RESPONSE; DEHYDRATION; DRUG DIFFUSION; EPIDERMIS; FEMALE; HIGH PERFORMANCE LIQUID CHROMATOGRAPHY; HUMAN; HUMAN CELL; HYDRATION; PRIORITY JOURNAL; SKIN HYDRATION METER; SKIN PENETRATION; STEADY STATE; STRATUM CORNEUM; THERMODYNAMICS; WATER CONTENT; ADULT; CHEMISTRY; DIFFUSION; DIFFUSION CHAMBER; IN VITRO STUDY; INTRADERMAL DRUG ADMINISTRATION; PH; SKIN ABSORPTION; SOLUTION AND SOLUBILITY;

ADMINISTRATION, CUTANEOUS; ADULT; DIFFUSION; DIFFUSION CHAMBERS, CULTURE; FEMALE; HUMANS; HYDROGEN-ION CONCENTRATION; IN VITRO TECHNIQUES; NICOTINE; NICOTINIC AGONISTS; PHARMACEUTICAL SOLUTIONS; PHARMACEUTICAL VEHICLES; SKIN ABSORPTION; THERMODYNAMICS;

EID: 84902135713     PISSN: 07248741     EISSN: 1573904X     Source Type: Journal    
DOI: 10.1007/s11095-013-1256-4     Document Type: Article

References (55)

1. Asmussen B. Transdermal therapeutic systems-actual state and future developments. Methods Find Exp Clin Pharmacol. 1991;13(5):343.
2. Michaels AS, Chandrasekaran SK, Shaw JE. Drug permeation through human skin: theory and in vitro experimental measurement. AIChE J. 1975;21(5):985-96.
3. Aronson JK. Nicotine replacement therapy. In: Aronson JK, editor. Meyler's side effects of drugs: the international encyclopedia of adverse drug reactions and interactions. Amsterdam: Elsevier; 2006. p. 2508-11.
4. Benowitz N, Hukkanen J, Jacob P. Nicotine chemistry, metabolism, kinetics and biomarkers. Handb Exp Pharmacol. 2009;192:29-60.
5. Domino E. Pharmacological significance of nicotine. In: John WG, Peyton III J, editors. Analytical determination of nicotine and related compounds and their metabolites. Amsterdam: Elsevier Science; 1999. p. 1-11.
6. Karnath B. Smoking cessation. Am J Med. 2002;112(5):399-405.
7. Wilson DJB. Nicotine poisoning by absorption through the skin. Br Med J. 1930;2(3640):601-2.
8. Lockhart LP. Nicotine poisoning. Br Med J. 1933;1(3762):246.
9. Faulkner JM. Nicotine poisoning by absorption through the skin. J Am Med Assoc. 1933;100(21):1664-5.
10. Rose J, Jarvik ME, Rose K. Transdermal administration of nicotine. Drug Alcohol depend. 1984;13(3):209-13.
11. Rose JE, Herskovic JE, Trilling Y, Jarvik ME. Transdermal nicotine reduces cigarette craving and nicotine preference. Clin Pharmacol Ther. 1985;38(4):450-6.
12. Bircher A, Howald H, Rufli T. Adverse skin reactions to nicotine in a transdermal therapeutic system. Contact Dermatitis. 1991;25(4):230-6.
13. Etscorn F. Transcutaneous application of nicotine. US Patent. 1986;4(597):961.
14. Baker R, Kochinke F, Huang C. Novel transdermal nicotine patch. US Patent. 1989;4(839):174.
15. Osborne J, Nelson M, Enscore D, Yum SI, Gale R. Subsaturated nicotine transdermal therapeutic system. US Patent. 1991;5(004):610.
16. Gupta S, Benowitz N, Jacob P, Rolf C, Gorsline J. Bioavailability and absorption kinetics of nicotine following application of a transdermal system. Br J Clin Pharmacol. 1993;36(3):221.
17. Fant R, Henningfield J, Shiffman S, Strahs K, Reitberg D. A pharmacokinetic crossover study to compare the absorption characteristics of three transdermal nicotine patches. Pharmacol Biochem Behav. 2000;67(3):479-82.
18. DeVeaugh-Geiss AM, Chen LH, Kotler ML, Ramsay LR, Durcan MJ. Pharmacokinetic comparison of two nicotine transdermal systems, a 21-mg/24-hour patch and a 25-mg/16-hour patch: A randomized, open-label, single-dose, two-way crossover study in adult smokers. Clin Therapeut. 2010;32(6):1140-8.
19. Zorin S, Kuylenstierna F, Thulin H. In vitro test of nicotine's permeability through human skin. Risk evaluation and safety aspects. Ann Occup Hyg. 1999;43(6):405-13.
20. Nair MK, Chetty DJ, Ho H, Chien YW. Biomembrane permeation of nicotine: Mechanistic studies with porcine mucosae and skin. J Pharm Sci. 1997;86(2):257-62.
21. Oakley D, Swarbrick J. Effects of ionization on the percutaneous absorption of drugs: partitioning of nicotine into organic liquids and hydrated stratum corneum. J Pharm Sci. 1987;76(12):866-71.
22. Aungst B. Nicotine skin penetration characteristics using aqueous & non-aqueous vehicles, anionic polymers, and silicone matrices. Drug Dev Ind Pharm. 1988;14(11):1481-94.
23. Roberts MS, Cross S, Pellett MA. Skin transport. In: Walters K, editor. Dermatological and transdermal formulations. 119: Informa healthcare; 2002. p. 89-194.
24. Jiang R, Roberts MS, Prankerd RJ, Benson HAE. Percutaneous absorption of sunscreen agents from liquid paraffin: self-association of octyl salicylate and effects on skin flux. J Pharm Sci. 1997;86(7):791-6.
25. Pellett MA, Roberts MS, Hadgraft J. Supersaturated solutions evaluated with an in vitro stratum corneum tape stripping technique. Int J Pharm. 1997;151(1):91-8.
26. Roberts MS. Solute-vehicle-skin interactions in percutaneous absorption: the principle and the people. Skin Pharmacol Physiol. 2013;26:356-70.
27. Dugard PH, Scott RC. A method of predicting percutaneous absorption rates from vehicle to vehicle: an experimental assessment. Int J Pharm. 1986;28:219-27.
28. Hudson CS. The mutual solubility of nicotine in water. Zeit Phys Chem. 1904;47(113).
29. Davies NSA, Gillard RD. The solubility loop of nicotine: water. Trans Met Chem. 2000;25:628-9.
30. Wiechers JW, Watkinson AC, Cross SE, Roberts MS. Predicting skin penetration of actives from complex cosmetic formulations: an evaluation of inter formulation and inter active effects during formulation optimization for transdermal delivery. Int J Cos Sci. 2012;34(6):525-35.
31. Kligman AM, Christophers E. Preparation of isolated sheets of human stratum corneum. Arch Dermatol. 1963;88(6):702-5.
32. Ho H, Chien YW. Kinetic evaluation of transdermal nicotine delivery systems. Drug Dev Ind Pharm. 1993;19(3):295-313.
33. Norton LB, Bigelow CR, Vincent WB. Partial vapour pressures from nicotine solutions at 25. NYSAES. 1940;345:261-4.
34. Barry BW, Harrison SM, Dugard PH. Correlation of thermodynamic activity and vapour diffusion through human skin for the model compound, benzyl alcohol. J Pharm Pharmacol. 1985;37:84-90.
35. Eberlein-König B, Schäfer T, Huss-Marp J, Darsow U, Möhrenschlager M, Herbert O, et al. Skin surface pH, stratum corneum hydration, trans-epidermal water loss and skin roughness related to atopic eczema and skin dryness in a population of primary school children: clinical report. Acta Derm Venereol. 2000;80(3):188-91. PubMed PMID: 3893232.
36. Barel A, Clarys P. In vitro calibration of the capacitance method (Corneometer CM 825) and conductance method (Skicon-200) for the evaluation of the hydration state of the skin. Skin Res Tech. 1997;3(2):107-13.
37. Cross SE, Pugh WJ, Hadgraft J, Roberts MS. Probing the effect of vehicles on topical delivery: understanding the basic relationship between solvent and solute penetration using silicone membranes. Pharm Res. 2001;18(7):999-1005.
38. Dias M, Hadgraft J, Lane ME. Influence of membrane-solvent-solute interactions on solute permeation in skin. Int J Pharm. 2007;340(1-2):65-70.
39. Blank IH. Penetration of low molecular-weight alcohols into skin I. Effect of concentration of alcohol and type of vehicle. J Invest Dermatol. 1964;43(5):415-20.
40. Roberts MS. Structure-permeability considerations in percutaneous absorption. In: Scott RC, Guy RH, Hadgraft J, Boddé HE, editors. Prediction of percutaneous penetration. London: IBC; 1991. p. 210-28.
41. Megrab NA, Williams AC, Barry BW. Oestradiol permeation through human skin and silastic membrane: effects of propylene glycol and supersaturation. J Controlled Release. 1995;36(3):277-94.
42. Johanson G, Fernström P. Influence of water on the percutaneous absorption of 2-butoxyethanol in guinea pigs. Scand J Work Env Hea. 1988;14(2):95-100.
43. Traynor M, Wilkinson S, Williams F. Corrigendum to "The influence of water mixtures on the dermal absorption of glycol ethers". Toxicol App Pharm. 2007;221(1):129.
44. Traynor M, Wilkinson S, Williams F. The influence of water mixtures on the dermal absorption of glycol ethers. Toxicol App Pharm. 2007;218(2):128-34.
45. Qvist M, Hoeck U, Kreilgaard B, Madsen F, Frokjaer S. Evaluation of Göttingen minipig skin for transdermal in vitro permeation studies. Eur J Pharm Sci. 2000;11(1):59-68.
46. Barry BW, Harrison SM, Dugard PH. Vapour and liquid diffusion of model penetrants through human skin; correlation with thermodynamic activity. J Pharm Pharmacol. 1985;37:226-35.
47. Pankow JF, Mader BT, Isabelle LM, Luo W, Pavlick A, Liang C. Conversion of Nicotine in tobacco smoke to its volatile and available free-base form through the action of gaseous ammonia. Environ Sci Technol. 1997;31(8):2428-33.
48. Bunge AL, Persichetti JM, Payan JP. Explaining skin permeation of 2-butoxyethanol from neat and aqueous solutions. Int J Pharm. 2012;435(1):50-62.
49. Bunge AL. Why skin permeation data from neat and aqueous solutions of 2-Buthoxythanol (BE) are not surprising. Perspective in Percutanous Penetration Poster. 2006.
50. Megrab NA, Williams AC, Barry BW. Oestradiol permeation across human skin, silastic and snake skin membranes: the effects of ethanol/water co-solvent systems. Int J Pharm. 1995;116(1):101-12.
51. Björklund S, Engblom J, Thuresson K, Sparr E. A water gradient can be used to regulate drug transport across skin. J Controlled Release. 2010;143(2):191-200.
52. Zhang Q, Li P, Roberts MS. Maximum transepidermal flux for similar size phenolic compounds is enhanced by solvent uptake into the skin. J Controlled Release. 2011;154(1):50-7.
53. Zhang Q, Grice JE, Li P, Jepps OG, Wang G-J, Roberts MS. Skin solubility determines maximum transepidermal flux for similar size molecules. Pharm Res. 2009;26(8):1974-85.
54. Oliveira G, Hadgraft J, Lane ME. The role of vehicle interactions on permeation of an active through model membranes and human skin. Int J Cos Sci. 2012;34(6):536-45.
55. Twist J, Zatz J. Influence of solvents on paraben permeation through idealized skin model membranes. J Cosmet Sci. 1986;37(6):429-44.