Evaluation of mechanical and mucoadhesive properties of clomiphene citrate gel formulations containing carbomers and their thiolated derivatives

Drug Delivery

Volumn 15, Issue 1, 2008, Pages 57-67

  Cevher, Erdal ^a   Taha, M A M ^b   Orlu, M ^a   Araman, A ^a  

^a ISTANBUL UNIVERSITY   (Turkey)

^b DG Pharmacy   (Sudan)

Author keywords

Clomiphene Citrate; Gel; Human Papilloma Virus; Polyacrylic Acid; Polyacrylic Acid Cysteine; Texture Profile Analysis; Vaginal Mucoadhesion

Indexed keywords

CARBOMER; CLOMIFENE CITRATE; POLYACRYLIC ACID; POLYMER; THIOL DERIVATIVE;

ARTICLE; DRUG ADSORPTION; DRUG DETERMINATION; DRUG FORMULATION; DRUG RELEASE; DRUG STABILITY; DRUG SYNTHESIS; ELASTICITY; HARDNESS; PH MEASUREMENT; PRIORITY JOURNAL; VAGINA MUCOSA;

ACRYLATES; ADHESIVENESS; ADMINISTRATION, INTRAVAGINAL; ANIMALS; ANTIVIRAL AGENTS; CATTLE; CHEMISTRY, PHARMACEUTICAL; CLOMIPHENE; COMPRESSIVE STRENGTH; CYSTEINE; DELAYED-ACTION PREPARATIONS; DRUG CARRIERS; DRUG COMPOUNDING; DRUG STABILITY; ELASTICITY; FEMALE; GELS; HARDNESS; HUMANS; KINETICS; MUCUS; PAPILLOMAVIRUS INFECTIONS; SOLUBILITY; VAGINA;

EID: 38149103499     PISSN: 10717544     EISSN: 15210464     Source Type: Journal    
DOI: 10.1080/10717540701829234     Document Type: Article

References (55)

1. Alur, H. H., Pather, S. I., Mitra, A. K., and Johnston, T. P. 1999. Transmucosal sustained-delivery of chlorpheniramine maleate in rabbits using a novel, natural mucoadhesive gum as an excipient in buccal tablets. Int. J. Pharm. 188:1-10.
2. Anlar, S., Çapan, Y. and Hincal, A. A. 1993. Physico-chemical and bioadhesive properties of polyacrylic acid polymers. Pharmazie 48:285-287.
3. Bernkop-Schn̈urch, A., Schwarz,V., and Steininger, S. 1999. Polymers with thiol groups: a new generation of mucoadhesive polymers? Pharm. Res. 16:876-881.
4. Bernkop-Schn̈urch, A. and Steininger, S. 2000. Synthesis and characterization of mucoadhesive thiolated polymers. Int. J. Pharm. 194:239-247.
5. Bernkop-Schn̈urch, A. Zarti, H., and Walker, G. F. 2001. Thiolation of polycarbophil enhances its inhibition of intestinal brush border membrane bound aminopeptidase. J. Pharm. Sci. 90:1907-1914.
6. Ceschel, G. C., Maffei, P., Lombardi, B. S., Ronchi, C., and Rossi, S. 2001a. Development of a mucoadhesive dosage form for vaginal administration. Drug Dev. Ind. Pharm. 27:541-547.
7. Ceschel, G. C., Maffei, P., and Lombardi. B. S. 2001b. Design and evaluation of a new mucoadhesive bi-layered tablet containing nimesulide for buccal administration. STP Pharm. Sci. 11:151-156.
8. Ceulemans, J., Vermeire, A., Adriaens, E., Remon, J. P., and Ludwig, A. 2001. Evaluation of a mucoadhesive tablet for ocular use. J. Control. Release 77:333-344.
9. Cevher, E., Sahin, O., and Araman, A. 2002. Investigations on topical formulations of clomiphene citrate for treatment of HPV lesion. Pharmazie 57:72-73.
10. Chang, J.Y., Oh,Y. K., Choi, H. G., Kim,Y. B., and Kim, C. K. 2002. Rheological evaluation of thermosensitive and mucoadhesive vaginal gels in physiological conditions. Int. J. Pharm. 241:155-163.
11. Chien, Y.W., and Lee, C.H. 2002. Drug delivery-vaginal route. In: Encyclopedia of Pharmaceutical Technology 2nd ed., Swarbrick J, and Boylan JC, pp. 961-985. Pinehurst, NC: PharmaceuTech, Inc., and Wilmington, NC: aaiPharma, Inc.
12. Choi, H. G., and Kim, C. K. 2000. Development of omeprazole buccal adhesive tablets with stability enhancement in human saliva. J. Control. Release 68:397-404.
13. Choi, H. G., Oh, Y. K., and Kim, C. K. 1998. In situ gelling and mucoadhesive liquid suppository containing acetaminophen: enhanced bioavailability. Int. J. Pharm. 165:23-32.
14. Czerwenka, K. F., Schön, H. J., Manavi, M., Zeillinger, R., Kubista, E., and Gitsch, E. 1991. Reliability of in-situ hybridization of smears and biopsies for papilloma virus genotyping of the uterina cervix. Eur. J. Clin. Chem. Clin. Biochem. 29:39-145.
15. Deshpande, A. A., Rhodes, C. T., and Danish, M. 1992. Intravaginal drug delivery. Drug Dev. Ind. Pharm. 18:1225-1279.
16. El-Kamel, A., Sokar, M., Naggar, V., and Gamal. S. A. 2002. Chitosan and sodium alginate-based bioadhesive vaginal tablets. AAPS Pharm. Sci. 4:1-7.
17. Gu, J. M., and Robinson, J. R. 1988. Binding of acrylic polymers to musin/epithelial surfaces: structure-property relationships. CRC Crit. Rev. Ther. Drug Carrier Syst. 5:21-67.
18. Han, R.Y., Fang, J. Y., Sung, K. C., and Hu, O. Y. P. 1999. Mucoadhesive buccal disks for novel nalbuphine prodrug controlled delivery: effect of formulation variables on drug release and mucoadhesive performance. Int. J. Pharm. 177:201-209.
19. Haşci̧cek, C., Gönül, N., and Erk, N. 2003. Mucoadhesive microspheres containing gentamicine sulfate for nasal administration: preparation and in vitro characterization. Il Farmaco 58:11-16.
20. Jimenez-Castellanos, R., Zia, H., and Rhodes, C. T. 1993. Mucoadhesive drug delivery systems. Drug Dev. Ind. Pharm. 19:143-194.
21. Jones, D. S., Irwin, C. R., Woolfson, A. D., Djokic, J., and Adams. V. 1999. Physicochemical characterization and preliminary in vivo efficiacy of bioadhesive, semisolid formulations containing flurbiprofen for the treatment of gingivitis. J. Pharm. Sci. 88:592-598.
22. Jones, D. S., Woolfson, A. D., and Brown, A. F. 1997a. Textural, viscoelastic and mucoadhesive properties of pharmaceutical gels composed of cellulose polymers. Int. J. Pharm. 151:223-233.
23. Jones, D. S.,Woolfson, A. D., Djokic, J., and Coulter.W.A. 1996a. Development and mechanical characterization of bioadhesive semi-solid, polymeric systems containing tetracycline for the treatment of periodontal diseases. Pharm. Res. 13:1734-1738.
24. Jones, D. S.,Woolfson, A. D., and Djokic, J. 1996b. Texture profiles analysis of bioadhesive polymeric semisolids: mechanical characterisation and investigation of interactions between formulation components. J. App. Polymer Sci. 16:2229-2234.
25. Jones, D. S., Woolfson, D. A., Brown, A. F., and O'Neill, M. J. 1997b. Mucoadhesive, syringeable drug delivery systems for controlled application of metronidazole to the periodontal pocket: in vitro release kinetics, syringeability, mechanical and mucoadhesive properties. J. Control. Release 49:71-79.
26. Kast, C. E., Valenta, C., Leopold, M., and Bernkop-Schnürch, A. 2002. Design and in vitro evaluation of a novel bioadhesive vaginal drug delivery system for clotrimazole. J. Control. Release 81:347-354.
27. Langoth, N., Kalbe, J., and Bernkop-Schnürch, A. 2003. Development of buccal drug delivery systems based on a thiolated polymer. Int. J. Pharm. 252:141-148.
28. Lee, C. H., and Chien, Y. W. 1996. Development and evaluation of a mucoadhesive drug delivery system for dual-controlled delivery Nonoxynol-9. J. Control. Release 39:93-103.
29. Maggi, L., Mastromarino, P., Macchia, S., Brigidi, P., Pirovano, F., Matteuzzi, D., and Conte, U. 2000. Technological and biological evaluation of tablets containing different strains of lactobacilli for vaginal administration. Eur. J. Pharm. Biopharm. 50:389-395.
30. McLeish, M. J. 1998. Clomiphene citrate. In: Analytical Profiles of Drug Substances and Excipients Florey, K. (Ed.), pp. 85-120. New York: Academic Press, Inc.
31. Noveon Pharmaceutical Bulletin 16: Bioadhesion, Cleveland Ohio: Noveon, Inc.
32. Park, H., and Robinson, J. R. 1985. Physico-chemical properties of water insoluble polymers important to mucin/epithelial adhesion. J. Control. Release 2:47-57.
33. Park, J. S., Oh, Y. K., Kang, M. J., and Kim, C. K. 2003. Enhanced mucosal and systemic immune responses following intravaginal immunization with human papilloma virus 16L1 virus-like particle vaccine in thermosensitive mucoadhesive delivery systems. J. Med. Virol. 70:633-641.
34. Pavelic, Z., Skalko-Basnet, N., and Schubert, R. 2001. Liposomal gels for vaginal drug delivery. Int. J. Pharm. 219:139-149.
35. Peppas, N. A., and Buri, P. A. 1985. Surface, interfacial and molecular aspects of polymer bioadhesion on soft tissues. J. Control. Release 2:257-275.
36. Perioli, L., Ambrogi, V., Rubini, D., Giovagnoli, S., Ricci, M., Blasi, P., and Rossi, C. 2004. Novel mucoadhesive buccal formulation containing metronidazole for the treatment of periodontal disease. J. Control. Release 95:521-533.
37. Richardson, J., and Illum, L. 1992. Routes of delivery: case studies, the vaginal route of peptide and protein drug delivery. Adv. Drug Del. Rev. 8:341-366.
38. Ryu, J. M., Chung, S. J., Lee, M. H., Kim, C. K., and Shim, C. K. 1999. Increased bioavailability of propranolol in rats by retaining thermally gelling liquid suppositories in the rectum. J. Control. release 59:163-172.
39. Sales, D., Sae-Lee, D., Matsuya, S., and Ana, I. D. 2003. Short-term fluoride and cations release from polyacid-modified composites in a distilled water, and an acidic lactate buffer. Biomaterials 24:1687-1696.
40. Schön, H. J., Czerwenka, K. F., Schurz, B., Kramar, R., and Kubista, E. 1991. Papanicolaou test and enzyme-linked in-situ hybridization a combined diagnostic system for papilloma virus infections with high prognostic value. Eur. J. Clin. Chem. Clin. Biochem. 29:131-138.
41. Schön, H.J., Grgurin, M., Szekeres, T., and Schurz, B. 1996. A new mode of treatment of human papilloma virus associated anogenital lesions using a nonsteroid estrogen analogue. Wien Klin. Wochenschr. 108:45-47.
42. Schwartz, N.O. 1975. Adaptation of sensory textile profile method to skin care products. J. Text. Studies 42:33-42.
43. Shin, S. C., Bum, J. P., and Choi, J. S. 2000. Enhanced bioavailability by buccal administration of triamcinolone acetonide from the bioadhesive gels in rabbits. Int. J. Pharm. 209:37-43.
44. Shojaei, A. H., Zhou, S. L., and Li, X. 1998. Transbuccal delivery of acyclovir (II): feasibility, system design, and in vitro permeation studies. J. Pharm. Pharmaceut. Sci. 1:66-73.
45. Smart, J. D., Kellaway, I. W., and Worthington, H. E. C. 1984. An in vitro investigation of mucosa adhesive materials for use in controlled drug delivery. J. Pharm. Pharmacol. 36:295-299.
46. Takeuchi, H., Matsui, Y., Yamamoto, H., and Kawashima, Y. 2003. Mucoadhesive properties of carbopol or chitosan-coated liposomes and their effectiveness in the oral administration of calcitonin to rats. J. Control. Release 86:235-242.
47. Tamburic, S., and Craig, D. Q. M. 1995. An investigation into the rheological, dielectric and mucoadhesive properties of poly (acrylic acid) gel systems . J. Control. Release 37:59-68.
48. Tan, Y. T. F., Peh, K. K., and Al-Hanbali, O. 2000. Effect of carpobol and polyvinylpyrrolidone on the mechanical, rheological and release properties of bioadhesive polyethylene glycol gels. AAPS PharmSciTech. 1:1-10.
49. Tobyn, M. J., Johnson, J. R., and Dettmar, P.W. 1995. Factors affecting in vitro gastric mucoadhesion I. Test Conditions and instrumental parameters. Eur. J. Pharm. Biopharm. 41:235-241.
50. Ugwoke, M. I., Sam, E., Mooter, G. V. D., Verbeke, N., and Kinget, R. 1999b. Nasal mucoadhesive delivery systems of the anti-parkinsonian drug, apomorphine: influence of drug-loading on in vitro and in vivo release in rabbits. Int. J. Pharm. 181:125-138.
51. U.S. Pharmacopeia, 24. Ed. 2000. Rockville, MD: United States Pharmacopeial Convention, Inc.
52. Valenta, C., Kast, C. E., Harich, I., and Bernkop-Schnürch, A. 2001. Development and in vitro evaluation of mucoadhesive vaginal delivery system for progesterone. J. Control. Release 77:323-332.
53. Yahagi, R., Machida, Y., Onishi, H., and Machida, Y. 2000. Mucoadhesive suppositories of ramosetron hydrochloride utilizing Carbopol®. Int. J. Pharm. 193:205-212.
54. Yahagi, R., Onishi, H., and Machida, Y. 1999. Preparation and evaluation of double-phased mucoadhesive suppositories of lidocaine utilizing Carbopol® and white beeswax. J. Control. Release 61:1-8.
55. Yun, M., Choi, H., Jung, J., and Kim, C. 1999. Development of a thermo-reversible insulin liquid suppository with bioavailability enhancement. Int. J. Pharm. 189(2):137-145.