Mukoadhezivní filmy jako perspektivní lékové formy pro orální podání
Authors:
Hana Landová; Zdeněk Daněk; Jan Gajdziok; David Vetchý; Jan Štembírek
Published in:
Čes. slov. Farm., 2013; 62, 4-11
Category:
Review Articles
Overview
Mukoadheze představuje specifický proces vytváření vazeb během těsného kontaktu mezi biologickými povrchy pokrytými slizovou vrstvou a mukoadhezivním materiálem. V posledních letech vstupují do popředí zájmu farmaceutického průmyslu moderní lékové formy založené na tomto procesu. Filmy složené z mukoadhezivních polymerů (deriváty celulosy, polyakryláty, polyoxyethylen atd.) připravené některou ze zavedených metod (odpařování rozpouštědla, extruze taveniny atd.) mohou být perspektivními kandidáty pro orální aplikaci mnoha léků, především pro jejich flexibilitu a pohodlné použití. K dalším výhodám této lékové formy patří zlepšení relativně krátké doby setrvání konvenčních orálních lékových forem na sliznici a dodání přesné dávky léčiva na místo aplikace. Kromě toho mohou také překrytím chránit povrch slizniční léze, což napomáhá ke snížení bolestivosti a zlepšení účinnosti léčby. Cílem tohoto článku je poskytnout přehled o principech vzniku mukoadhezivních vazeb a o inovativní lékové formě – mukoadhezivních filmech z hlediska jejich složení, přípravy a praktického využití.
Klíčová slova:
sliznice dutiny ústní • principy mukoadheze • mukoadhezivní lékové formy • filmy • disky
Sources
1. Smart J. D. The basics and underlying mechanism of mucoadhesion. Adv. Drug Deliv. Rev. 2005; 57, 1556–1568.
2. Peppas N. A., Sahlin J. J. Hydrogels as mucoadhesive and bioadhesive materials: a review. Biomaterials 1996; 17, 1553–1561.
3. Longer M. A., Robinson J. R. Fundamental apects of bioadhesion. Pharm. Int. 1986; 7, 114–117.
4. Chickering D. E., Mathiowitz E. Definitions, mechanisms, and theories of bioadhesion. In: Mathiowitz, E., Chickering, D. E., Lehr, C. M. eds. Bioadhesive drug delivery systems: Fundamentals, novel approaches, and developement. 1st ed. New York: Marcel Dekker Inc. 1999.
5. Duchźne D., Touchard F., Peppas N. A. Pharmaceutical and medical aspects of bioadhesive systems for drug administration. Drug Dev. Ind. Pharm. 1988; 14, 283–318.
6. Serra L., Doménech J., Peppas N. A. Engineering design and molecular dynamics of mucoadhesive drug delivery systems as targeting agents. Eur. J. Pharm. Biopharm. 2009; 71, 519–528.
7. Derjaguin B. V., Aleinikova I. N., Toporov Y. P. On the role of electrostatic forces in the adhesion of polymer particles to solid surfaces. Progr. Surf. Sci. 1994; 45, 119–123.
8. Kinloch A. J. The science of adhesion: Part 2 Mechanics and mechanisms of failure. J. Mater. Sci. 1982; 17, 617–651.
9. Kealble D. H., Moacanin J. A surface energy analysis of bioadhesion. Polymer. 1977; 18, 475–482.
10. Wake W. C. Theories of adhesion and uses of ahesives: a review. Polymer. 1978; 19, 291–308.
11. Ahagon A., Gent A. N. Effect of interfacial bonding on the strength of adhesion. J. Polymer. Sci. Polymer. Phys. Ed. 1975; 13, 1285–1300.
12. Lehr C. M., Bouwstra J. A., Boddé H. E., Junginger H. E. A surface energy analysis of mucoadhesion: Contact angle measurements on polycarbophil and pig intestinal mucosa in physiologically relevant fluids. Pharm. Res. 1992; 9, 70–75.
13. Sudhakar Y., Kuotsu K., Bandyopadhyay A. K. Buccal bioadhesive drug delivery – A promising option for orally less efficient drugs. J. Contr. Release. 2006; 114, 15–40.
14. Salamat-Miller N., Chittchang M., Johnston T. P. The use of mucoadhesive polymers in buccal drug delivery. Adv. Drug Deliv. Rev. 2005; 57, 1666–1691.
15. Nafee N. A., Boraie M. A., Ismail F. A., Mortada L. M. Design and characterization of mucoadhesive buccal patches containing cetylpyridinium chloride. Acta Pharm. 2003; 53, 199–212.
16. McQuinn R. L., Kvam D. C., Maser M. J., Miller A. L., Oliver S. Sustained oral mucosal delivery in human volunteers of buprenorphine from a thin non-eroding mucoadhesive polymeric disk. J. Contr. Release. 1995; 34, 243–250.
17. Robinson J. R., Lomger M. A., Veillard M. Bioadhesive polymers for controlled drug delivery. Ann. NY. Acad. Sci. 1987; 507, 307–314.
18. Lee J. W., Park J. H., Robinson J. R. Bioadhesive-based dosage forms: The next generation. J. Pharm. Sci. 2000; 89, 850–866.
19. Roy S. K., Prabhakar B. Bioadhesive polymeric platforms for transmucosal drug delivery systems – a review. Trop. J. Pharm. Res. 2010; 9, 91–104.
20. Bernkop-Schnürch A., Schwarz V., Steininger S. Polymer with thiol groups: A new generation of mucoadhesive polymers? Pharm. Res. 1999; 16, 876–881.
21. Lehr C-M. Lectin-mediated drug delivery: The second generation of bioadhesives. J. Control. Release. 2000; 65, 19–29.
22. Dixit R. P., Puthli S. P. Oral strip technology: Overview and future potential. J. Control. Release. 2009; 139, 94–107.
23. Ganem-Quintanar A., Kalia Y. N., Falson-Rieg F., Buri P. Mechanisms of oral permeation enhancement. Int. J. Pharm. 1997; 156, 127–142.
24. Veuillez F., Kalia Y. N., Jacques Y., Deshusses J., Buri P. Factors and strategies for improving buccal absorption of peptides. Eur. J. Pharm. Biopharm. 2001; 51, 93–109.
25. Lueßen H. L., Lehr C.-M., Rentel C.-O., Noach A. B. J., de Boer A. G., Verhoef J. C., Junginger H. E. Bioadhesive polymers for the peroral delivery of peptide drugs. J. Control. Release. 1994; 29, 329–338.
26. Morales J. O., McConville J. T. Manufacture and characterization of mucoadhesive buccal films. Eur. J. Pharm. Biopharm. 2011; 77, 187–199.
27. Repka M. A., Repka S. L., McGinity J. W. Bioadhesive hot-melt extruded film for topical and mucosal adhesion applications and drug delivery and process for preparation thereof. US Patent Office, Patent No 6375963 B1. 2002.
28. Chokshi R., Zia H. Hot melt extrusion technique: A review. Iran J. Pharm. Res. 2004; 3, 3–16.
29. Repka M. A., Koleng J. J., Zhang F. Hot-melt extrusion technology. In: Swarbrick, J., Boylan, J. C. eds. Encyclopedia of Pharmaceutical Technology, 2nd ed. New York: Marcel Dekker Inc. 2002.
30. Alur H. H., Johnston T. P., Mitra A. K. Peptides and proteins: Buccal absorption. In: Swarbrick, J., Boylan, J. C. eds. Encyclopedia of Pharmaceutical Technology, 2nd ed. New York: Marcel Dekker Inc. 2002.
31. Gandhi R. B., Robinson J. R. Oral cavity as a site for bioadhesive drug delivery. Adv. Drug Deliv. Rev. 1994; 13, 43–74.
32. Burgalassi S., Panichi L., Saettone M. F., Jacobsen J., Rassing M. R. Development and in vitro/in vivo testing of mucoadhesive buccal patches releasing benzydamine and lidocaine. Int. J. Pharm. 1996; 133, 1–7.
33. Ikinci G., Senel S., Akincibay H., Kas S., Ercis S., Wilson C. G., Hincal A. A. Effect of chitosan on a periodontal pathogen Porphyromonas gingivalis. Int. J. Pharm. 2002; 235, 121–127.
34. Jones D. S., Medlicott N. J. Casting solvent controlled release of chlorhexidine from ethylcellulose films prepared by solvent evaporation. Int. J. Pharm. 1995; 114, 257–261.
35. Senel S., Ikinci G., Kas S., Yousefi-Rad A., Sargon M. F., Hincal A. A. Chitosan films and hydrogels of chlorhexidine gluconate for oral mucosal delivery. Int. J. Pharm. 2000; 193, 197–203.
36. Choudhury A., Das A., Dhangar S., Kapasiya S., Kanango A. Development and characterization buccoadhesive film of ciprofloxacin hydrochloride. Int. J. PharmTech. Res. 2010; 2, 1050–1057.
37. Repka M. A., Prodduturi S., Stodghill S. P. Production and characterization of hot-melt extruded films containing clotrimazole. Drug Dev. Ind. Pharm. 2003; 29, 757–765.
38. Mura P., Corti G., Cirri M., Maestrelli F., Mennini N., Bragagni M. Development of mucoadhesive films for buccal administration of flufenamic acid: Effect of cyclodextrin complexation. J. Pharm. Sci. 2010; 99, 3019–3029.
39. Perioli L., Ambrogi V., Angelici F., Ricci M., Giovagnoli S., Capuccella M., Rossi C. Development of mucoadhesive patches for buccal administration of ibuprofen. J. Contr. Release. 2004; 99, 73–82.
40. Perugini P., Genta I., Conti B., Modena T., Pavanetto F. Periodontal delivery of ipriflavone: new chitosan/PLGA film delivery system for a lipophilic drug. Int. J. Pharm. 2003; 252, 1–9.
41. Kohda Y., Kobayashi H., Baba Y., Yuasa H., Ozeki H., Kanay Y., Sagara E. Controlled release of lidocaine hydrochloride from buccal mucosa-adhesive films with solid dispersion. Int. J. Pharm. 1997; 158, 147–155.
42. Okamoto H., Taguchi H., Iida K., Danjo K. Development of polymer film dosage forms of lidocaine for buccal administration: I. Penetration rate and release rate. J. Contr. Release. 2001; 77, 253–260.
43. Okamoto H., Taguchi H., Iida K., Danjo K. Development of polymer film dosage forms of lidocaine for buccal administration: II. Comparison of preparation methods. J. Pharm. Sci. 2002; 91, 2424–2432.
44. Varshosaz J., Karimzadeh S. Development of cross-linked chitosan films for oral mucosal delivery of lidocaine. Res. Pharm. Sci. 2007; 2, 43–52.
45. Ishida M., Nambu N., Nagai T. Mucosal dosage form of lidocaine for toothache using hydroxypropyl cellulose and carbopol. Chem. Pharm. Bull. (Tokyo) 1982; 30, 980–984.
46. Repka M. A., Gutta K., Prodduturi S., Munjal M., Stodghill S. P. Characterization of cellulosic hot-melt extruded films containing lidocaine. Eur. J. Pharm. Biopharm. 2005; 59, 189–196.
47. Shah D., Gaud R. S., Misra A. N. Formulation of a water soluble mucoadhesive film of lycopene for treatment of leukoplakia. Int. J. Pharmaceut. Sci. Rev. Res. 2010; 2, 6–10.
48. Nafee N. A., Ismail F. A., Boraie N. A., Mortada L. M. Mucoadhesive buccal patches of miconazole nitrate: in vitro/in vivo performance and effect of ageing. Int. J. Pharm. 2003; 264, 1–14.
49. Aksungur P., Sungur A., Ünal S., Iskit A. B., Alper B., Squier C. A., Senel S. Chitosan delivery systems for treatment of oral mucositis: in vitro and in vivo studies. J. Contr. Release. 2004; 98, 269–279.
50. Llabot J. M., Palma S. D., Manzo R. H. Allemandi D. A. Design of novel antifungal mucoadhesive films: Part I. Pre-formulation studies. Int. J. Pharm. 2007; 330, 54–60.
51. Llabot J. M., Palma S. D., Manzo R. H. Allemandi D. A. Design of novel antifungal mucoadhesive films: Part II. Formulation and in vitro biopharmaceutical evaluation. Int J Pharm 2007 336: 263–268.
52. Boateng J. S., Auffret A. D., Matthews K. H., Humphrey M. J., Stevens H. N. E., Eccleston G. M. Characterization of freeze-dried wafers and solvent evaporated films as potential drug delivery systems to mucosal surfaces. Int. J. Pharm. 2010; 389, 24–31.
53. Oguchi M., Shikama N., Sasaki S., Gomi K., Katsuyama Y., Ohta S., Hori M., Takei K., Arakawa K., Sone S. Mucosa-adhesive water-soluble polymer film for treatment of acute radiation-induced oral mucositis. Int. J. Radiat. Oncol. Biol. Phys. 1998; 40, 1033–1037.
54. Agarwal R. K., Robinson D. H., Maze G. I., Reinhardt R. A. Development and characterization of tetracycline-poly (lactide/glycolide. films for treatment of periodontitis. J. Contr. Realese. 1993; 23, 137–146.
55. Donnelly F. A., McCarron P. A., Tunney M. M., Woolfson A. D. Potential of photodynamic therapy in treatment of fungal infections of the mouth: Design and characterisation of a mucoadhesive patch containing toluidine blue O. J. Photochem. Photobiol. B. Biol. 2007; 86, 59–69.
56. Ahn J. S., Choi H. K., Chun M. K., Ryu J. M., Jung J. H., Kim Y. U., Choa C. S. Release of triamcinolone acetonide from mucoadhesive polymer composed of chitosan and poly(acrylic acid) in vitro. Biomaterials. 2002; 23, 1411–1416.
57. Chun M. K, Kwak B. T., Choi H. K. Preparation of buccal patch composed of carbopol, poloxamer and hydroxypropyl methylcellulose. Arch. Pharm. Res. 2003; 26, 973–978.
58. Kim T. H., Ahn J. S., Choi H. K., Choi Y. J., Cho C. S. A novel mucoadhesive polymer film composed of Carbopol, poloxamer and hydroxypropylmethylcellulose. Arch. Pharm. Res. 2007; 30, 381–386.
59. Shojaei A. R., Berner B., Li X. Transbuccal delivery of acyclovir: I. In vitro determination of routes of buccal transport. Pharm. Res. 1998; 15, 1182–1188.
60. Shojaei A. R., Zhou S., Li X. Transbuccal delivery of acyclovir: II. Feasibility, system design, and in vitro permeation studies. J. Pharm. Pharmaceut. Sci. 1998; 1, 66–73.
61. Rossi,S., Sandri G., Ferrari F., Bonferoni M. C., Caramella C. Buccal delivery of acyclovir from films based on chitosan and polyacrylic acid. Pharmaceut. Dev. Tech. 2003; 8, 199–208.
62. Guo J-H. Bioadhesive polymer buccal patches for buprenorphine controlled delivery: Formulation, in vitro adhesion and release properties. Drug Dev. Ind. Pharm. 1994; 20, 2809–2821.
63. Guo J-H, Cooklock K. M. Bioadhesive polymer buccal patches for buprenorphine controlled delivery: Solubility consideration. Drug Dev. Ind. Pharm. 1995; 21, 2013–2019.
64. Thimmasetty J., Pandey G. S., Sathes Babu P. R. Design and in vivo evaluation of carvedilol buccal mucoadhesive patches. Pak. J. Pharm. Sci. 2008; 21, 1–8.
65. Choudhary A., Tiwari G., Pandey M., Kymonil K. M., Saraf S. A. Formulation and characterization of carvedilol buccal mucoadhesive patches. Int. J. Res. Pharmaceut. Sci. 2010; 1, 396–401.
66. Tiwari D., Sause R., Madan P. L. Evaluation of polyoxyethylene homopolymers for buccal bioadhesive drug delivery device formulations. AAPS PharmSci. 1999; 1, 1–8.
67. Semalty A., Bhojwani M., Bhatt G. K., Gupta G. D., Shrivastav A. K. Design and evaluation of mucoadhesive buccal films of diltiazem hydrochloride. Indian J. Pharmaceut. Sci. 2005; 67, 548–552.
68. Manish K., Garima G., Pushpendra K. Design and in vitro evaluation of mucoadhesive buccal films containing famotidine. Int. J. Pharm. Pharmaceut. Sci. 1990; 2, 86–90.
69. Diaz del Consuelo I., Falson F., Guy R. H., Jacques Y. Ex vivo evaluation of bioadhesive films for buccal delivery of fentanyl. J. Contr. Release. 2007; 112, 135–140.
70. Subrahmanyam C. V. S., Thimmasetty J., Manish Kumar D. S., Manjunath K., Shivanand K., et al. Design and evaluation of fexofenadine HCl buccal mucoadhesive patches. Biomed. 2007; 2, 78–83.
71. Ilango R., Kavimani S., Mullaicharam A. R., Jayakar B. In-vitro studies on buccal strips of glibenclamide using chitosan. Indian J. Pharmaceut. Sci. 1997; 59, 232–235.
72. Semalty M., Semalty A., Kumar G., Juyal V. Development of mucoadhesive buccal films of glipizide. Int. J. Pharmaceut. Sci. Nanotechnology. 2008; 1, 184–190.
73. Ritschel W. A., Ritschel G. B., Forusz H., Kraeling M. Buccal absorption of insulin in the dog. Res. Commun. Chem. Pathol. Pharmacol. 1989; 63, 53–67.
74. Doijad R. C., Manvi F. V., Malleswara Rao V. S. N., Patel P. S. Buccoadhesive drug delivery system of isosorbide dinitrate: Formulation and evaluation. Indian J. Pharmaceut. Sci. 2006; 68, 744–748.
75. Koland M., Charyulu R. N., Prabhu P. Mucoadhesive films of losartan potassium for buccal delivery: Design and characterization. Indian J. Pharm. Educ. Res. 2010; 44, 315–323.
76. Wong C. F., Yuen K. H., Peh K. K. Formulation and evaluation of controlled release Eudragit buccal patches. Int. J. Pharm. 1999; 178, 11–22.
77. Save T., Shah M. U., Ghamande A. R. Comparative study of bucoadhesive formulations and sublingual capsules of nifedipine. J. Pharm. Pharmacol. 1994; 46, 192–195.
78. RemuĖán-López C., Portero A., Vila-Jato J. L., Alonso M. J. Design and evaluation of chitosan/ethylcellulose mucoadhesive bilayered devices for buccal drug delivery. J. Contr. Release. 1998; 55, 143–152.
79. Nappinnai M., Chandanbala R., Balaijirajan R. Formulation and evaluation of nitrendipine buccal films. Indian J. Pharmaceut. Sci. 2008; 70, 631–635.
80. Li C., Bhatt P. P., Johnston T. P. In vitro release and permeation of oxytocin from mucoadhesive buccal patch. Pharmaceut. Dev. Tech. 1996; 1, 357–364.
81. Li C., Bhatt P. P., Johnston T. P. Transmucosal delivery of oxytocin to rabbits using a mucoadhesive buccal patch. Pharmaceut. Dev. Tech. 1997; 2, 265–274.
82. Basu B., Garala K., Thimmasetty J. Formulation and evaluation of pimozide buccal muccoadhesive patches. Int. J. Pharmaceut. Sci. Nanotechnology. 2010; 2, 739–748.
83. Cui Z., Mumper R. J. Bilayer films for mucosal (genetic. immunization via the buccal route in rabbits. Pharmaceut. Res. 2002; 19, 947–953.
84. Patel V. M., Prajapati B. G., Patel M. M. Effect of hydrophilic polymers on buccoadhesive eudragit patches of propranolol hydrochloride using factorial design. AAPS PharmSciTech. 2007; 8, E1–E8.
85. Anders R., Merkle H. P. Evaluation of laminated muco-adhesive patches for buccal drug delivery. Int. J. Pharm. 1989; 3, 231–240.
86. Patel R. S., Poddar S. S. Development and characterization of mucoadhesive buccal patches of salbutamol sulphate. Curr. Drug. Deliv. 2009; 6, 140–144.
87. Pavan Kumar G. V., Ramakrishna V., William G. J., Konde A. Formulation and evaluation of buccal films of salbutamol sulphate. Indian J. Pharmaceut. Sci. 2005; 67, 160–164.
88. Cui Z., Mumper R. J. Buccal transmucosal delivery of calcitonin in rabbits using thin-film composites. Pharmaceut. Res. 2002; 19, 1901–1906.
89. Pramodkumar T. M., Shivakumar H. G. Novel core in cup buccoadhesive systems and films of terbutaline sulphate – development and in vitro evaluation. Asian J. Pharmaceut. Sci. 2006; 1, 175–187.
90. Jay S., Fountain W., Cui Z., Mumper R. J. Transmucosal delivery of testosterone in rabbits using novel bi-layer mucoadhesive wax-film composite disks. J. Pharm. Sci. 2002; 91, 2016–2025.
91. Li C., Koch R. L., Raul V. A., Bhatt P. P., Johnston T. P. Absorption of Thyrotropin-releasing hormone in rats using a mucoadhesive buccal patch. Drug Dev. Ind. Pharm. 1997; 23, 139–246.
Labels
Pharmacy Clinical pharmacologyArticle was published in
Czech and Slovak Pharmacy
![Issue 1](https://www.prolekare.cz/media/cache/resolve/journal_issue/media/image_pdf/7e953bd6a7518fffd4184c79e3d673a9.jpeg)
2013 Issue 1
Most read in this issue
- Pediatrické perorální roztoky s propranolol-hydrochloridem pro magistraliter přípravu: formulace a hodnocení stability
- Orální mukóza a léčba rekurentní aftózní stomatitidy
- Mukoadhezivní filmy jako perspektivní lékové formy pro orální podání
- Organizácia a riadenie znárodneného farmaceutického priemyslu so zameraním na Slovensko od roku 1945 do roku 1948