Triggered in situ drug supersaturation and hydrophilic matrix self-assembly

Pharmaceutical Research

Volumn 29, Issue 12, 2012, Pages 3434-3442

  Benaouda, F ^a   Brown, M B ^b   Martin, G P ^a   Jones, S A ^a  

^a KING'S COLLEGE LONDON   (United Kingdom)

^b MEDPHARM LTD   (United Kingdom)

Author keywords

Diclofenac; Hydrophilic matrix; Non ideal mixing; Solvent solvent interaction; Supersaturation; Topical drug delivery; Transmembrane transport

Indexed keywords

ALCOHOL; DICLOFENAC; HYDROXYPROPYLMETHYLCELLULOSE; MACROGOL; SOLVENT; WATER;

ARTICLE; DRUG PENETRATION; DRUG SOLUBILITY; DRUG TRANSPORT; EMBEDDING; EVAPORATION; HYDROPHILICITY; MEMBRANE TRANSPORT; PHARMACOKINETICS; PHARMACOLOGICAL PARAMETERS; PHYSICAL CHEMISTRY; PRIORITY JOURNAL; SUPRAMOLECULAR CHEMISTRY; THERMODYNAMICS;

ANTI-INFLAMMATORY AGENTS, NON-STEROIDAL; CRYSTALLIZATION; DICLOFENAC; ETHANOL; HYDROPHOBIC AND HYDROPHILIC INTERACTIONS; METHYLCELLULOSE; PROPYLENE GLYCOL; SOLUBILITY; THERMODYNAMICS;

EID: 84872076448     PISSN: 07248741     EISSN: 1573904X     Source Type: Journal    
DOI: 10.1007/s11095-012-0838-x     Document Type: Article

References (37)

1. Davis AF, Hadgraft J. Effect of supersaturation on membrane transport: 1. Hydrocortisone acetate. Int J Pharm. 1991;76(1-2):1-8.
2. Megrab NA, Williams AC, Barry BW. Oestradiol permeation through human skin and silastic membrane: effects of propylene glycol and supersaturation. J Contr Release. 1995;36(3):277-94.
3. Schwarb FP, Imanidis G, Smith EW, Haigh JM, Surber C. Effect of concentration and degree of saturation of topical fluocinonide formulations on in vitro membrane transport and in vivo availability on human skin. Pharm Res. 1999;16(6):909-15. (Pubitemid 29284204)
4. Higuchi T. Physical chemical analysis of percutaneous absorption process from creams and ointments. J Soc Cosmet Chem. 1960;11:85-97.
5. Iervolino M, Cappello B, Raghavan SL, Hadgraft J. Penetration enhancement of ibuprofen from supersaturated solutions through human skin. Int J Pharm. 2001;212(1):131-41. (Pubitemid 32121958)
6. Leichtnam ML, Rolland H, Wuthrich P, Guy RH. Impact of antinucleants on transdermal delivery of testosterone from a spray. J Pharm Sci. 2007;96(1):84-92. (Pubitemid 46087341)
7. Brown MB, and Jones SA. Topical formulations. [WO2007031753]. 2007.
8. Reed BL., Morgan TM, Finnin BC. Dermal penetration enhancers and drug delivery systems involving same. [6818226]. 2004.
9. Reid ML, Brown MB, Jones SA. Manipulation of corticosteroid release from a transiently supersaturated topical metered dose aerosol using a residual miscible co-solvent. Pharm Res. 2008;25(11):2573-80.
10. Reid ML, Jones SA, Brown MB. Transient drug supersaturation kinetics of beclomethasone dipropionate in rapidly drying films. Int J Pharm. 2009;371(1-2):114-9.
11. Jones SA, Reid ML, Brown MB. Determining degree of saturation after application of transiently supersaturated metered dose aerosols for topical delivery of corticosteroids. J Pharm Sci. 2009;98(2):543-54.
12. Smyth HDC. The influence of formulation variables on the performance of alternative propellant-driven metered dose inhalers. Adv Drug Deliv Rev. 2003;55(7):807-28. (Pubitemid 36776795)
13. Van Wesenbeeck I, Driver J, Ross J. Relationship between the evaporation rate andvapor pressure of moderately and highly volatile chemicals. Bull Environ Contam Toxicol. 2008;80(4):315-8.
14. Vervaet C, Byron PR. Drug-surfactant-propellant interactions in HFA-formulations. Int J Pharm. 1999;186(1):13-30. (Pubitemid 29397519)
15. Bairamov DE, Chalykh AE, Feldstein MM, Siegel RA. Impact of molecular weight on miscibility and interdiffusion between poly (N-vinyl pyrrolidone) and poly (ethylene glycol). Macromol Chem Phys. 2002;203(18):2674-85.
16. Walkow JC, Mcginity JW. The effect of physicochemical properties on the in vitro diffusion of drug through synthetic membranes and Pigskin. 1. Methyl Salicylate. Int J Pharm. 1987;35(1-2):91-102. (Pubitemid 17016882)
17. Sasutjarit R, Sirivat A, Vayumhasuwan P. Viscoelastic properties of Carbopol 940 gels and their relationships to piroxicam diffusion coefficients in gel bases. Pharm Res. 2005;22(12):2134-40. (Pubitemid 41821593)
18. Di Colo G, Carelli V, Giannaccini B. Vehicle effects in percutaneous absorption: In vitro study of influence of solvent power and microscopic viscosity of vehicle on benzocaine release from suspension hydrogels. J Pharm Sci. 1980;69(4):387-91. (Pubitemid 10079745)
19. Herkenne C, Naik A, Kalia YN, Hadgraft J, Guy RH. Effect of propylene glycol on ibuprofen absorption into human skin in vivo. J Pharm Sci. 2008;97(1):185-97.
20. Watkinson RM, Guy RH, Hadgraft J, Lane ME. Optimisation of Cosolvent Concentration for Topical Drug Delivery - II: Influence of Propylene Glycol on Ibuprofen Permeation. Skin Pharmacol Physiol. 2009;22(4):225-30.
21. Benaouda F, Brown MB, Ganguly S, Jones SA, Martin GP. Discriminating the molecular identity and function of discrete supramolecular structures in topical pharmaceutical formulations. Mol Pharm. 2012. doi:10.1021/mp300127f.
22. Benaouda F. A study of in situ supersaturation for skin delivery. Thesis, (PhD). King's College London. 2010.
23. Williams RO, Liu J. Influence of formulation additives on the vapor pressure of hydrofluoroalkane propellants. Int J Pharm. 1998;166(1):99-103. (Pubitemid 28239743)
24. Wensink EJW. Dynamic properties of water/alcohol mixtures studied by computer simulation. J Chem Phys. 2003;119:7308-18.
25. Chickos JS, Acree WE. Enthalpies of vaporization of organic and organometallic compounds, 1880-2002. J Phys Chem Ref Data. 2003;32(2):519-878. (Pubitemid 36814426)
26. Noskov S, Lamoureux G, Roux B. Molecular Dynamics Study of Hydration in Ethanol-Water Mixtures Using a Polarizable Force Field. J Phys Chem B. 2005;109(14):6705-13. (Pubitemid 40538438)
27. Pecar D, Dolecek V. Volumetric properties of ethanol-water mixtures under high temperatures and pressures. Fluid Phase Equilibr. 2005;230(1-2):36-44. (Pubitemid 40572745)
28. Li A, Yalkowsky SH. Solubility of Organic Solutes in Ethanol-Water Mixtures. J Pharm Sci. 1994;83(12):1735-40.
29. Dixit S, Crain J, Poon WCK, Finney JL, Soper AK. Molecular segregation observed in a concentrated alcohol-water solution. Nature. 2002;416:829-32. (Pubitemid 34453735)
30. Frank HS, Evans MW. Free volume and entropy in condensed systems. III. Entropy in binary liquid mixtures; partial molal entropy in dilute solutions; structure and thermodynamics in aqueous electrolytes. J Chem Phys. 1945;13:507-32.
31. Franks F, Ives DJG. The structural properties of alcohol-water mixtures. Q Rev. 1966;20:1-45.
32. Tanaka H, Gubbins K. Structure and thermodynamic properties of water-methanol mixtures. J Chem Phys. 1992;97:2626-34.
33. Rubino JT, Obeng EK. Influence of solute structure on deviations from the log-linear solubility equation in propylene glycol: water mixtures. J Pharm Sci. 1991;80(5):479-83.
34. Smith CC, Lof G, Jones R. Measurement and analysis of evaporation from an inactive outdoor swimming pool. Solar Energ. 1994;53(1):3-7.
35. Leichtnam ML, Rolland H, Wuthrich P, Guy RH. Enhancement of transdermal testosterone delivery by supersaturation. J Pharm Sci. 2006;95(11):2373-9. (Pubitemid 44726378)
36. Raghavan SL, Trividic A, Davis AF, Hadgraft J. Effect of cellulose polymers on supersaturation and in vitro membrane transport of hydrocortisone acetate. Int J Pharm. 2000;193(2):231-7. (Pubitemid 30001867)
37. Yalkowsky SH, Valvani SC, Amidon GL. Solubility of nonelectrolytes in polar-solvents.4. Nonpolar drugs in mixed solvents. J Pharm Sci. 1976;65(10):1488-94.