In vitro and ex vivo bioadhesivity analysis of polymeric intravaginal caplets using physicomechanics and computational structural modeling

International Journal of Pharmaceutics

Volumn 370, Issue 1-2, 2009, Pages 151-159

  Ndesendo, Valence M K ^a   Pillay, Viness ^a   Choonara, Yahya E ^a   Khan, Riaz A ^b   Meyer, Leith ^a   Buchmann, Eckhart ^c   Rosin, Uwe ^d  

^a UNIVERSITY OF THE WITWATERSRAND   (South Africa)

^b INTEGRAL UNIVERSITY   (India)

^c UNIVERSITY OF THE WITWATERSRAND   (South Africa)

^d Research and Development Unit   (South Africa)

Author keywords

Bioadhesion; Bioadhesive polymers; Excised rabbit vaginal tissue; Intravaginal drug delivery; Structural modeling; Textural profile analysis

Indexed keywords

CARBOMER; CARRAGEENAN; MACROGOL; PENTAERYTHRITOL; PENTAERYTHRITYL TETRANITRATE; POLYACRYLIC ACID; POLYAMIDE; POLYGLACTIN; RESOMER; SUCROSE;

ANIMAL TISSUE; ARTICLE; CAPLET; CHEMICAL STRUCTURE; CHEMOMETRIC ANALYSIS; CROSS LINKING; DRUG DOSAGE FORM; DRUG MIXTURE; DRUG STRUCTURE; DRY POWDER; EX VIVO STUDY; FEMALE; IN VITRO STUDY; NONHUMAN; PHYSICAL CHEMISTRY; POLYMERIZATION; PRIORITY JOURNAL; SHEAR STRESS; STRUCTURE ANALYSIS; VAGINA;

ACRYLIC RESINS; ADHESIVENESS; ADMINISTRATION, INTRAVAGINAL; ANIMALS; CHEMISTRY, PHARMACEUTICAL; COMPUTER SIMULATION; DRUG DELIVERY SYSTEMS; FEMALE; MATERIALS TESTING; POLYMERS; RABBITS; RHEOLOGY; TABLETS; VISCOSITY;

EID: 61349119919     PISSN: 03785173     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.ijpharm.2008.12.001     Document Type: Article

References (49)

1. Al-Tahami K., and Singh J. Smart polymer based delivery systems for peptides and proteins. Recent Patents Drug Deliv. Formulation 1 (2007) 65-71
2. Bilensoy E., Rouf M.A., Vural I., Sen M., and Hincal A.A. Mucoadhesive, thermosensitive, prolonged-release vaginal gel for clotrimazole: β-cyclodestrin complex. AAPS PharmSciTech. 7 (2006) 38
3. Bogentoft, C., Carlsson, A., 1996. Gel forming liquid carrier composition, US Patent 5,492,937. http://www.freepatentsonline.com/5492937.html (accessed May 16, 2008).
4. Bonferoni M.C., Giunchedi P., Scalia S., et al. Chitosan gels for the vaginal delivery of lactic acid: relevance of formulation parameters to mucoadhesion and release mechanisms. AAPS PharmSciTech. 7 (2006) E1-E8
5. Ceschel G.C., Maffei P., Lombardi B.S., Ronchi C., and Rossi S. Development of a mucoadhesive dosage form for vaginal administration. Drug Dev. Ind. Pharm. 6 (2001) 541-547
6. Deryaguin B.V., Toporov Y.P., Mueler V.M., and Aleinikova I.N. On the relationship between the electrostatic and molecular component of the adhesion of elastic particles to a solid surface. J. Colloid Interf. Sci. 58 (1997) 528-533
7. Desphande A., Rhodes C.T., and Danish M. Intravaginal drug delivery. Drug Dev. Ind. Pharm. 18 (1992) 1225-1279
8. Elson C., Milne A., Curran D., and Kydonieus A.N. O-carboxymethylchitosan as a mucoadhesive for vaginal delivery of levonorgestrel. Proc. Int. Symp. Control Rel. Bioact. Mater. 27 (2000) 7201-7202
9. Furuhjelm M., Karlgren C., and Carlstrom K. Intravaginal administration of conjugated estrogens in postmenopausal women. Int. J. Gynecol. Obstet. 17 (1980) 335-339
10. Genc L., Oguzlar C., and Güler E. Studies on vaginal bioadhesive tablets of acyclovir. Pharmazie 55 (2000) 297-299
11. +. Food Hydrocolloids 17 (2003) 723-737
12. +. Food Hydrocolloids 17 (2003) 739-749
13. Gilsenan P.M., Richardson R.K., and Morris E.R. Associative and seggregative interactions between gelation and low methoxy pectin. Part III. Quantitative analysis of co-gel moduli. Food Hydrocolloids 17 (2003) 751-761
14. Helfand E., and Tagami Y. Theory of the interface between immiscible polymers. J. Chem. Phys. 57 (1972) 1812-1815
15. Hussain N. Bioadhesive drug delivery systems: fundamentals, novel approaches and development. Int. J. Pharm. 205 (2000) 201-202
16. Jast B., Li X., and Clearly G. Recent advances in mucoadhesive drug delivery systems. Drug Deliv. Polym. 1 (2003) 194-196
17. Kaelble D.H. A surface energy analysis of bioadhesion. Polymer 18 (1977) 475-482
18. - salvation shells in liquid DMSO: molecular dynamics simulations. J. Mol. Liq. 91 (2001) 135-148
19. Kast C.E., Valenta C., Leopold M., and Bernkop-Schnürch A. Design and in vitro evaluation of a novel bioadhesive vaginal drug delivery system for clotrimazole. J. Control Rel. 81 (2002) 347-354
20. Kolawole O.A., Pillay V., and Choonara Y.E. Novel polyamide 6,10 variants synthesized by modified interfacial polymerization for application as a rate-modulated monolithic drug delivery System. J. Bioact. Comp. Polym. 22 (2007) 281-313
21. Lee W.J., Park J.H., and Robinson J.R. Biodhesive-based dosage forms: the next generation. Am. Pharm. Assoc. J. Pharm. Sci. 89 (2000) 850-866
22. Lehr C.M. Lectin-mediated drug delivery: the second generation of bioadhesive. J. Control Rel. 65 (2000) 19-29
23. Longer M.A., and Robinson J.R. Fundamental aspects of bioadhesion. Pharm. Int. 7 (1986) 114-117
24. Mandal T.K. Swelling-controlled release system for the vaginal delivery of miconazole. Eur. J. Pharm. Biopharm. 50 (2000) 337-343
25. Mikos A.G., and Peppas N.A. Proceed. Int. Symp. Control Rel. Bioact. Mater. 13 (1986) 97
26. Mikos A.G., and Peppas N.A. Scaling concepts and molecular theories of the adhesion of synthetic polymers to glycoproteins. In: Lenaerts V., and Gurny R. (Eds). Bioadhesive Drug Delivery Systems (1990), CRC Press, Boca Raton, FL 25-42
27. Nelson, A.L., 2008. The vagina: new options for the administration of medications. http://www.medscape.com/viewarticle/504375_6 (accessed March 10).
28. Park K. A new approach to study mucoadhesion: colloidal gold staining. Int. J. Pharm. 53 (1989) 209-217
29. Park K., and Robinson J.R. Bioadhesive polymers as platforms for oral controlled drug delivery: method to study bioadhesion. Int. J. Pharm. 19 (1984) 107-127
30. Park H., and Robinson J.R. Mechanisms of mucoadhesion of poly(acrylic acid) hydrogels. Pharm. Res. 4 (1987) 457-464
31. Peppas N.A., and Buri P.A. Surface, interfacial and molecular aspects of polymer bioadhesion on soft tissues. J. Control Rel. 2 (1985) 257-275
32. ++ induced gelation of low methoxy pectin in the presence of oxidized starch. Part I. Collapse of network structure. Carbohydrate Polym. 43 (2000) 113-122
33. Picout D.R., Richardson R.K., and Morris E.R. Co-gelation of calcium pectinate with potato maltodextrin. Part I. Network formation on cooling. Carbohydrate Polym. 43 (2000) 133-141
34. Repka M.A., and McGinity J.W. Bioadhesive properties of hydroxyproplycellulose topical films produced by hot-melt extrusion. J. Control Rel. 70 (2001) 341-351
35. Robinson, J.R., Bologna, W.J., 2002. Use of polycarboxylic acid polymers to treat vaginal infections, US Patent 6,017,521. http://www.freepatentsonline.com/6017521.html (accessed March 15, 2008).
36. Santos C.A., Jacob J.S., Hertzog B.A., et al. Correlation of two bioadhesive assays: the averted sac technique and the CAHN microbalance. J. Control Rel. 61 (1999) 113-122
37. Schroeder G., Leska B., and Brzezinski B. Solvent effect for proton transfer reaction from dimethyl(4-nitrophenyl)malonate to cis 1,2-bis(dimethylaminomethyl) cyclohexane. J. Mol. Struct. 446 (1998) 235-239
38. Semalty, A., Semalty, M., 2008. Mucoadhesive polymers-a review. http://www.pharmainfo.net/reviews/mucoadhesive-polymers-review (accessed February 28, 2008).
39. Smart J.D., and Kellaway I.W. In vitro techniques for measuring mucoadhesion. J. Pharm. Pharmacol. 34 (1982) 70-170
40. Smart J.D., Kellaway I.W., and Worthington H.E.C. An in vitro investigation of muco-adhesive materials for use in controlled delivery. J. Pharm. Pharmacol. 36 (1984) 295-299
41. Steinberg M.S. Adhesion in development: An historical overview. Dev. Biol. 180 (1996) 377-388
42. ® solution (SPHCcs): synthesis, characterization and in vitro bioadhesive force studies. Eur. Polym. J. 41 (2005) 557-562
43. Ugwoke M.I., Exaud S., Van Den Mooter G., Verbeke N., and Kinget R. Bioavailability of apomorphine following intranasal administration of mucoadhesive drug delivery systems in rabbits. Eur. J. Pharm. Sci. 9 (1999) 213-219
44. Valenta C. The use of mucoadhesive polymers in vaginal delivery. Adv. Drug Deliv. Rev. 57 (2005) 1692-1712
45. Valenta C., Kast C.E., Harich I., and Bernkop-Schnürch A. Development and in vitro evaluation of a mucoadhesive vaginal delivery system for progesterone. J. Control Rel. 77 (2001) 323-332
46. Valenta C., Marschütz M., Egyed C., and Bernkop-Schnürch A. Evaluation of the inhibitory effect of thiolated poly(acrylates) on vaginal membrane bound aminopeptidase. J. Pharm. Pharmacol. 54 (2002) 603-610
47. Vermani K., and Garg S. The scope and potential of vaginal drug delivery. Pharm. Sci. Tech. Today (PSTT) 3 (2000) 359-364
48. ® buccal patches. Int. J. Pharm. 178 (1999) 11-22
49. Yu Z., and Quinn P.J. Solvation effects of dimethyl sulfoxide on the structure of phospholipids bi-layers. Biophys. Chem. 70 (1998) 35-39