Supersaturation as a Galenic Concept for Improving the Cutaneous Bioavailability of Drugs in Topical Therapy.
Cutaneous bioavailability
Galenics
Supersaturation
Journal
Dermatology and therapy
ISSN: 2193-8210
Titre abrégé: Dermatol Ther (Heidelb)
Pays: Switzerland
ID NLM: 101590450
Informations de publication
Date de publication:
Feb 2023
Feb 2023
Historique:
received:
27
10
2022
accepted:
05
12
2022
pubmed:
22
12
2022
medline:
22
12
2022
entrez:
21
12
2022
Statut:
ppublish
Résumé
The essential force that allows an epicutaneously applied drug to penetrate the skin is mediated by diffusion. The physicochemical properties of the skin tissue at the site of application and the concentration gradient of the dissolved drug between the vehicle and the stratum corneum are decisive here. One way to specifically improve these diffusion conditions is to use supersaturation. This uses the physical principle of the difference between the solubility curve and precipitation curve (Ostwald-Miers range). During the conversion of the application vehicle into the segregation vehicle, supersaturation of the dissolved drug substance in a solvent is achieved by evaporation, e.g., of a solubilizer. In principle, the change in solubility can also be achieved by heating and then cooling a solution. This principle has already been realized in a formulation of a fixed combination of calcipotriol and betamethasone dipropionate, two lipophilic drugs susceptible to hydrolysis, and is available on the market as a spray foam.
Identifiants
pubmed: 36542293
doi: 10.1007/s13555-022-00873-0
pii: 10.1007/s13555-022-00873-0
pmc: PMC9884713
doi:
Types de publication
Journal Article
Review
Langues
eng
Pagination
391-398Informations de copyright
© 2022. The Author(s).
Références
Ludwig W-D, Mühlbauer B, Seifert RE. Arzneimittelverordnungs-Report 2021. Springer Verlag; 2022.
Wohlrab J, Staubach P, Augustin M, Eisert L, Hunerbein A, Nast A, Reimann H, Stromer K, Mahler V. S2k-Leitlinie zum Gebrauch von Praparationen zur lokalen Anwendung auf der Haut (Topika). J Dtsch Dermatol Ges. 2018;16:376–92.
Wohlrab J. Grundlagen der topischen therapie. Hautarzt. 2014;65:169–74.
doi: 10.1007/s00105-013-2654-6
Wohlrab J, Klauck D, Savtcheva E. Regulatorische besonderheiten von topika. Hautarzt. 2014;65:175–9.
doi: 10.1007/s00105-013-2655-5
Wohlrab J. Influence of keratolytics on cutaneous pharmacokinetics of glucocorticoids. J Dtsch Dermatol Ges. 2021;19:554–61.
Wohlrab J. Topicals and their use in dermatology. J Dtsch Dermatol Ges. 2016;14:1061–71.
Surber C, Knie U. Metamorphosis of vehicles: mechanisms and opportunities. Curr Probl Dermatol. 2018;54:152–65.
doi: 10.1159/000489529
Scheuplein RJ. Mechanism of percutaneous absorption. II. Transient diffusion and the relative importance of various routes of skin penetration. J Invest Dermatol. 1967;48:79–88.
doi: 10.1038/jid.1967.11
der Justiz B. Gesetz über den verkehr mit arzneimitteln (arzneimittelgesetz—AMG). BGBl. 2005;I:4530.
Herman A, Herman AP. Essential oils and their constituents as skin penetration enhancers for transdermal drug delivery: a review. J Pharm Pharmacol. 2015;67:473–85.
doi: 10.1111/jphp.12334
Chattaraj SC, Walker RB. Penetration enhancer classification. In: Smith EW, Maibach HI, editors. Percutaneous penetration enhancers. CRC Press; 1995. p. 5–20.
Yang M, Gong W, Wang Y, Shan L, Li Y, Gao C. Bioavailability improvement strategies for poorly water-soluble drugs based on the supersaturation mechanism: an update. J Pharm Sci. 2016;19:208–25.
Edueng K, Mahlin D, Grasjo J, Nylander O, Thakrani M, Bergstrom CAS. Supersaturation potential of amorphous active pharmaceutical ingredients after long-term storage. Molecules. 2019;24:2731.
doi: 10.3390/molecules24152731
Coe FL, Clark C, Parks JH, Asplin JR. Solid phase assay of urinary cystine supersaturation in the presence of cystine binding drugs. J Urol. 2001;166:688–93.
doi: 10.1016/S0022-5347(05)66044-2
Sarode AL, Wang P, Obara S, Worthen DR. Supersaturation, nucleation, and crystal growth during single- and biphasic dissolution of amorphous solid dispersions: polymer effects and implications for oral bioavailability enhancement of poorly water soluble drugs. Eur J Pharm Biopharm. 2014;86:351–60.
doi: 10.1016/j.ejpb.2013.10.005
Cilurzo F, Casiraghi A, Selmin F, Minghetti P. Supersaturation as a tool for skin penetration enhancement. Curr Pharm Des. 2015;21:2733–44.
doi: 10.2174/1381612821666150428125046
Moser K, Kriwet K, Froehlich C, Kalia YN, Guy RH. Supersaturation: enhancement of skin penetration and permeation of a lipophilic drug. Pharm Res. 2001;18:1006–11.
doi: 10.1023/A:1010948630296
Lebwohl M, Tyring S, Bukhalo M, Alonso-Llamazares J, Olesen M, Lowson D, Yamauchi P. Fixed combination aerosol foam calcipotriene 0.005% (Cal) plus betamethasone dipropionate 0.064% (BD) is more efficacious than Cal or BD aerosol foam alone for psoriasis vulgaris: a randomized, double-blind, multicenter, three-arm, phase 2 study. J Clin Aesthet Dermatol. 2016;9:34–41.
Koo J, Tyring S, Werschler WP, Bruce S, Olesen M, Villumsen J, Bagel J. Superior efficacy of calcipotriene and betamethasone dipropionate aerosol foam versus ointment in patients with psoriasis vulgaris—a randomized phase II study. J Dermatolog Treat. 2016;27:120–7.
doi: 10.3109/09546634.2015.1083935
Paul C, Stein- Gold L, Cambazard F, Kalb RE, Lowson D, Bang B, Griffiths CEM. Cacipotriol plus betamethasone dipropionate aerosol foam provides superior efficacy vs gel in patients with psoriasis vulgaris: randomized, controlled PSO-ABLE study. J Eur Acad Dermatol Venereol. 2017;31:119–26.
doi: 10.1111/jdv.13859
Griffiths CE, Stein Gold L, Cambazard F, Kalb RE, Lowson D, Moller A, Paul C. Greater improvement in quality of life outcomes in patients using fixed-combination calcipotriol plus betamethasone dipropionate aerosol foam versus gel: results from the PSO-ABLE study. Eur J Dermatol. 2018;28:356–63.
doi: 10.1684/ejd.2018.3302
Mattozzi C, Salvi M, D’Epiro S, Giancristoforo S, Macaluso L, Luci C, Lal K, Calvieri S, Richetta AG. Importance of regulatory T cells in the pathogenesis of psoriasis: review of the literature. Dermatology. 2013;227:134–45.
doi: 10.1159/000353398
Jannin V. Complex interplay between solubilization, digestion, supersaturation and absorption of poorly soluble drugs with lipid-based formulations. Curr Drug Deliv. 2018;15:749–51.
doi: 10.2174/1567201814666171018120817
Raina SA, Zhang GG, Alonzo DE, Wu J, Zhu D, Catron ND, Gao Y, Taylor LS. Impact of solubilizing additives on supersaturation and membrane transport of drugs. Pharm Res. 2015;32:3350–64.
doi: 10.1007/s11095-015-1712-4
Hirakawa Y, Ueda H, Takata Y, Minamihata K, Wakabayashi R, Kamiya N, Goto M. Co-amorphous formation of piroxicam-citric acid to generate supersaturation and improve skin permeation. Eur J Pharm Sci. 2021;158: 105667.
doi: 10.1016/j.ejps.2020.105667
Inoue K, Ogawa K, Okada J, Sugibayashi K. Enhancement of skin permeation of ketotifen by supersaturation generated by amorphous form of the drug. J Control Release. 2005;108:306–18.
doi: 10.1016/j.jconrel.2005.08.008