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2015 | 28 | 4 | 225-230
Tytuł artykułu

The influence of hydrophylic polymers on the release rate of calcium dobesilate in hydrogel formulation assessed in vitro using porcine ear skin

Treść / Zawartość
Warianty tytułu
Języki publikacji
EN
Abstrakty
EN
A shortage of available experimental data exists in the available bibliography on the release rate of calcium dobesilate (CD) from hydrogel formulations. Thus, the aim of the study was to evaluate the effect of selected hydrophilic nonionic polymers and anionic polymers on the release rate of CD from formulation provided for dermal application, as compared to the reference product in the market. The work utilized excised pork skin, while, Methylcellulose (MC), hydroxypropyl methylcellulose (HPMC), and anionic polymers (copolymers of acrylic acid) were used as CD carriers. The release study was executed by the pharmacopoeial paddle method, with extraction cells and fresh excised porcine skin as a membrane. CD in aqueous acceptor fluid was quantified by UV-VIS spectrometry at 300 nm. Subsequently, the kinetic curves were fitted to a zero-order kinetics model, a first-order kinetics model, a second-order kinetics model, as well as to the Higuchi model. The work saw that porcine ear skin influences the release pattern of the CD, compared to the artificial membrane. In the study, the evaluated formulations with MC, polyacrylic acid (PA) and polyacrylate crosspolymer 11 (PC-11) deliver over 60% of the active component (AC), within 250 min, through the excised porcine ear skin, to the acceptor compartment. Moreover, the release observed via porcine ear skin to the aqueous acceptor compartment is congenial to zero-order or first-order kinetics. In addition, the formulations prepared on the basis of MC and PA appear to control AC delivery, independently of actual concentration of AC.
Wydawca

Rocznik
Tom
28
Numer
4
Strony
225-230
Opis fizyczny
Daty
wydano
2015-12-01
otrzymano
2015-10-21
zaakceptowano
2015-11-18
online
2015-12-30
Twórcy
  • Department of Physical Chemistry, Wroclaw Medical University, Faculty of Pharmacy, Borowska 211A, 50-556 Wroclaw, Poland
autor
  • Department of Physical Chemistry, Wroclaw Medical University, Faculty of Pharmacy, Borowska 211A, 50-556 Wroclaw, Poland
autor
  • Department of Physical Chemistry, Wroclaw Medical University, Faculty of Pharmacy, Borowska 211A, 50-556 Wroclaw, Poland
  • Department of Physical Chemistry, Wroclaw Medical University, Faculty of Pharmacy, Borowska 211A, 50-556 Wroclaw, Poland
  • Department of Physical Chemistry, Wroclaw Medical University, Faculty of Pharmacy, Borowska 211A, 50-556 Wroclaw, Poland, witold.musial@umed.wroc.pl
Bibliografia
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  • 3. Brunet J. et al.: Angioprotective action of calcium dobesilate against reactive oxygen species-induced capillary permeability in the rat. Eur. J. Pharmacol. 358, 213, 1998.
  • 4. Cuevas P. et al.: Dobesilate is an angiogenesis inhibitor. Eur. J. Med. Res., 10, 369, 2005.
  • 5. Cuevas P. et al.: Topical dobesilate eye drops for ophthalmic primary pterygium. BMJ Case Rep. 2012 Mar 8;2012. pii: bcr1220115449. doi: 10.1136/bcr.12.2011.5449.
  • 6. Cuevas P. et al.: Treatment of Stargardt disease with dobesilate. BMJ Case Rep. 2012 Oct 12;2012. pii: bcr2012007128. doi: 10.1136/ bcr-2012-007128..
  • 7. Cuevas P., Arrazola J. M.: Treatment of basal cell carcinoma with dobesilate. J. Am. Dermatol., 53, 526, 2005.
  • 8. Dash S. et al.: Kinetic modeling on drug release from controlled drug delivery system. Acta Pol. Pharm. 67, 217, 2010.
  • 9. Dick I. P., Scott R. C.: Pig Ear Skin as an In-vitro Model for Human Skin Permeability. J. Pharm. Pharmacol., 44, 640, 1992.
  • 10. European Pharmacopoeia 7.0, 2.9.4: Dissolution test for transdermal patches, 01/2008:20904, 2011.
  • 11. Fuchs E., Raghavan S.: Getting under the skin of epidermal morphogenesis. Nature Rev. Gen., 3, 199, 2002.[Crossref]
  • 12. Genç L., Oğuzlar C., Güler E.: Studies on vaginal bio-adhesive tablets of acyclovir. Pharmazie, 55, 297, 2000.
  • 13. Graber R. et al.: Calcium Dobesilate protects human peripheral blood mononuclear cells from oxidation and apoptosis. Apoptosis, 3, 41, 1998.
  • 14. Hamishehkar H. et al.: The Relationship between Solubility and Transdermal Absorption of Tadalafil. Adv. Pharm. Bull., 5, 411, 2015.[Crossref]
  • 15. Herkenne C. et al.: Pig ear skin ex-vivo as a model for in vivo dermatopharmacokinetic studies in man. Pharm. Res., 23, 1850, 2006.[Crossref]
  • 16. Hu G. et al.: Selective electrochemical sensing of calcium dobesilate based on an ordered mesoporous carbon-modified pyrolytic graphite electrode. J. Electroanal. Chem., 633, 264, 2009.[WoS]
  • 17. Iriz E. et al.: Effects of calcium dobesilate and diosmin-hesperidin on apoptosis of venous wall in primary varicose veins. Vasa, 37, 233, 2008.[WoS]
  • 18. Jacobi U. et al.: Porcine ear skin: an in-vitro model for human skin. Skin Res. Technol., 13, 19, 2007.[Crossref][WoS]
  • 19. Jafferany M. et al.: Geriatric dermatoses: a clinical review of skin diseases in an aging population. Int. J. Dermatol., 51, 509, 2012.[WoS]
  • 20. Kaur C. et al.: An open trial of calcium dobesilate with venous ulcers and stasis dermatitis. Int. J. Dermatol., 42, 147, 2003.[Crossref]
  • 21. Kendall M. et al.: Effects of Relative Humidity and Ambient Temperature on the Ballistic Delivery of Micro-Particles to Excised Porcine Skin. J. Investig. Dermatol., 122, 739, 2004.
  • 22. Kong R., Bhargava R.: Characterization of porcine skin as a model for human skin studies, using infrared spectroscopic imaging. Analyst, 136, 2359, 2011.[WoS]
  • 23. Lisik A. et al.: Effect of standard and reversible arrangements of Ph.Eur./USP extraction cells during dissolution tests of calcium dobesilate in hydrogel formulation. Curr. Issues Pharm. Med. Sci., 28, 136, 2015.
  • 24. Morimoto N. et al.: The Rapid Inactivation of Porcine Skin by Applying High Hydrostatic Pressure without Damaging the Extracellular Matrix. BioMed Res. Int., 2015, Article ID 587247, 2015.
  • 25. Reddy D. N. et al.: Design, development and characterization of clopidogrel bisulfate transdermal drug delivery system - Asian J. Pharm. Clin. Res., 8, 277, 2015.
  • 26. Rota R. et al.: Reduction of retinal albumin leakage by the antioxidant calcium dobesilate in streptozotocin-diabetic rats. Eur. J.Pharmacol., 495, 217, 2004.
  • 27. Ruiz E., Lorente R., Tejerina T.: Effects of calcium dobesilate on the synthesis of endothelium-dependent relaxing factors in rabbit isolated aorta. Brit. J. Pharmacol., 121, 711, 1997.
  • 28. Sekkat N., Kalia Y.N., Guy R.H.: Porcine Ear Skin as a Model for the Assessment of Transdermal Drug Delivery to Premature Neonates. Pharm. Res., 21, 1390, 2004.[Crossref]
  • 29. Siepmann J., Peppas N. A.: Modeling of drug release from delivery systems based on hydroxypropyl methylcellulose (HPMC). Adv. Drug Deliv. Rev., 48, 139, 2001.[WoS][Crossref]
  • 30. Summerfield A., Meurens F., Ricklin M.E.: The immunology of the porcine skin and its value as a model for human skin. Molec. Immunol., 66, 14, 2015.
  • 31. Suschek C., Kolb H., Kolb-Bachofen V.: Dobesilate enhances endothelial nitric oxide synthase-activity in macro- and microvascular endothelial cells. Brit. J. Pharmacol., 122, 1502, 1997.
  • 32. Tejerina T., Ruiz E.: Calcium Dobesilate: Pharmacology and Future Approaches. Gen. Pharmacol., 31, 357, 1998.[Crossref]
  • 33. Žilius M., Ramanauskienė K., Briedis V.: Release of Propolis Phenolic Acids from Semisolid Formulations and Their Penetration into the Human Skin In Vitro, J. Evid. Based Complementary Altern. Med., 2013, Article ID 958717, 2013, doi:10.1155/2013/958717.[Crossref]
Typ dokumentu
Bibliografia
Identyfikatory
Identyfikator YADDA
bwmeta1.element.-psjd-doi-10_1515_cipms-2015-0076
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