Vaginal gel drug delivery systems: Understanding rheological characteristics and performance

Expert Opinion on Drug Delivery

Volumn 8, Issue 10, 2011, Pages 1309-1322

  Yu, Tao ^a   Malcolm, Karl ^a   Woolfson, David ^a   Jones, David S ^a   Andrews, Gavin P ^a  

^a QUEEN'S UNIVERSITY BELFAST   (United Kingdom)

Author keywords

Gels; Rheological methods; Vaginal drug delivery

Indexed keywords

ESTROGEN; EXCIPIENT; GLYCEROL; POLYACRYLIC ACID; POLYMER; WATER;

DRUG COATING; DRUG DELIVERY SYSTEM; DRUG DESIGN; DRUG FORMULATION; DRUG SCREENING; GEL; HUMAN; MENSTRUATION; PH; REVIEW; SCIENTIST; SPERM; STORAGE; VAGINAL GEL DRUG DELIVERY SYSTEM; VISCOELASTICITY; VISCOSITY;

ADMINISTRATION, INTRAVAGINAL; DRUG DELIVERY SYSTEMS; FEMALE; GELS; HUMANS; RHEOLOGY;

EID: 80053087983     PISSN: 17425247     EISSN: 17447593     Source Type: Journal    
DOI: 10.1517/17425247.2011.600119     Document Type: Review

References (77)

1. das Neves J, Bahia MF. Gels as vaginal drug delivery systems. Int J Pharm 2006; 318: 1-14 (Pubitemid 43963297)
2. Vermani K, Garg S. The scope and potential of vaginal drug delivery. Pharm Sci Technol Today 2000;3:359-64
3. Hussain A, Ahsan F. The vagina as a route for systemic drug delivery. J Control Release 2005;103:301-13 (Pubitemid 40342532)
4. Ross-Murphy SB. Rheological characterisation of gels. J Texture Stud 1995a;26:391-400 (Pubitemid 126019481)
5. Tsitsilianis C. Responsive reversible hydrogels from associative "smart" macromolecules. Soft Matter 2010;6:2372-88
6. Nijenhius K. Viscoelastic properties of thermoreversible gels. In: Burchard W, Ross-Murphy SB. editors. Physical networks. Elsevier; London: 1990
7. Hernandez MJ, Pellicer J, Delegidio J, et al. Rheological characterisation of easy to disperse (ETD) Carbopol hydrogels. J Dispersion Sci Technol 1998;19:31-42
8. Ghannam MT, Esmail MN. Rheological properties of carboxymethylcellulose. J Appl Polym Sci 1997;64:289
9. Durand D, Bertand C, Busnel JP, et al. Physical gelation induced by ionic complexation: pectin-calcium systems. In: Burchard W, Ross-Murphy SB. editors. Physical Networks. Elsevier; London: 1990
10. Garg S, Tambwekar KR, Vermani K, et al. Compendium of pharmaceutical excipients for vaginal formulations. Pharm Technol 2001;14-24. Available at http://pharmtech.findpharma.com/pharmtech/data/articlestandard//pharmtech/ 512001/5133/article.pdf (Last accessed 1 July 2011) (Pubitemid 33051614)
11. Owen DH, Peters JJ, Kieweg SL, et al. Biophysical analysis of prototype microbicidal gels. J Pharm Sci 2007;96:661-9 (Pubitemid 46466086)
12. Barnhart KT, Pretorius SE, Timbers K, et al. Distribution of a 3.5-mL (1.0%) C31G vaginal gel using magnetic resonance imaging. Contraception 2005;71:357-61 (Pubitemid 40602314)
13. Curran RM, Donnelly L, Morrow JR, et al. Vaginal delivery of the recombinant HIV-1 clade-C trimeric gp140 envelope protein CN54gp140 within novel rheologically structured vehicles elicits specific immune responses. Vaccine 2009;27:6791-8
14. Lai BE, Xie YQ, Lavine ML, et al. Dilution of microbicide gels with vaginal fluid and semen simulants: effect on rheological properties and coating flow. J Pharm Sci 2008;97:1030-8 (Pubitemid 351293901)
15. Baloglu E, Senyigit ZA, Karavana SY, et al. Strategies to prolong the intravaginal residence time of drug delivery system. J Pharm Pharm Sci 2009;3:312-36
16. Pendergrass P, Belovicz M, Reeves C. Surface area of the human vagina as measured from vinyl polysiloxane casts. Gynecol Obstet Invest 2003;55:110-13 (Pubitemid 36667680)
17. Weber A, Walters M, Schover L. Vaginal anatomy and sexual function. Obstet Gynecol 1995;86:946-9 (Pubitemid 27331490)
18. Alexander NJ, Baker E, Kaptein M, et al. Why consider vaginal drug administration? Fertil Steril 2004;82:1-12 (Pubitemid 38968766)
19. Burkitt HG, Young B, Heath JW. Histologia Funcional. 3rd edition. Guanabara Koogan, RJ; Rio de Janeiro: 1994
20. Szeri AJ, Park SC, Verguet S, et al. A model of transluminal flow of an anti-HIV microbicide vehicle:combined elastic squeezing and gravitational sliding. Phys Fluids 2008;20:83101
21. Owen DH, Peters JJ, Lavine ML, et al. Effect of temperature and pH on contraceptive gel viscosity. Contraception 2003;67:57-64 (Pubitemid 36084290)
22. Dasari S, Pereira L, Reddy AP, et al. Comprehensive proteomic analysis of human cervical-vaginal fluid. J Proteome Res 2007;6:1258-68 (Pubitemid 46724022)
23. Rathbone MJ. Intravaginal drug delivery technologies. In: Rathbone MJ. editor. Modified-release Drug Delivery Technology. Volume 2. Chapter 35 2nd edition. 2008
24. Levin RJ. Vagina, clitoral and periure-thral glans-an update on human female genital arousal. Exp Clin Endocrinol 1991;98:61-9
25. Verguet S, Holt BY, Szeri AJ. Increasing the effectiveness of vaginal microbicides: a biophysical framework to rethink behavioral acceptability. PLoS ONE 2010;5:1-8
26. Ness RB, Hillier SL, Richter HE, et al. Douching in relation to bacterial vaginosis, lactobacilli, and facultative bacteria in the vagina. Obstet Gynecol 2002;100:765-72 (Pubitemid 35300036)
27. Liu Y, Zhu Y-Y, Wei G, et al. Effect of carrageenan on poloxamer-based in situ gel for vaginal use: improved in vitro and in vivo sustained-release properties. Eur J Pharm Sci 2009;37:306-12
28. Aka-Any-Grah A, Bouchemal K, Koffi A, et al. Formulation of mucoadhesive vaginal hydrogels insensitive to dilution with vaginal fluids. Eur J Pharm Biopharm 2010;76:296-303
29. Hombachi J, Palmberger TF, Bernkop-Schnurch A. Development and in vitro evaluation of a mucoadhesive vaginal delivery system for nystatin. J Pharm Sci 2009;98:555-64
30. Jones DS, Woolfson DA, Brown AF, et al. Design, characterisation and preliminary clinical evaluation of a novel mucoadhesive topical formulation containing tetracycline for the treatment of periodontal disease. J Control Release 2000;67:357-68 (Pubitemid 30303848)
31. Gunasekaran S, Ak MM. Dynamic oscillatory shear testing of foods-selected application. Trends Food Sci Technol 2000;11:115-27 (Pubitemid 32035614)
32. Coviello T, Coluzzi G, Palleschi A, et al. Strutural and rheological charaterization of Scleroglucan/borax hydrogel for drug delivery. Int J Biol Macromol 2003;32:83-92 (Pubitemid 37040663)
33. Jones DS, Bruschi ML, Freitas OD, et al. Rheological, mechanical and mucoadhesive properties of thermoresponsive, bioadhesive binary mixtures composed of poloxamer 407 and carbopol 974P designed as platforms for implantable drug delivery systems for use in the oral cavity. Int J Pharm 2009;372:49-58
34. Jones DS, Woolfson DA, Brown AF. Viscoelastic properties of bioadhesive chlorhexidine-containing semi-solids for topical application to the oropharynx. Pharm Res 1998;15:1131-6 (Pubitemid 28356934)
35. Hu X, Fan J, Yue CY. Rheological study of crosslinking and gelation in bismaleimide/cyanate ester interpenetrating polymer network. J Appl Polym Sci 2001;80:2437-45
36. Tamburic S, Craig DQ, Vuleta G, et al. An investigation into the use of thermrheology and texture analysis in the evaluation of W/O creams stabilized with a silicone emulsifier. Pharm Dev Technol 1996b;3:299-306
37. Andrews GP, Donnelly L, Jones DS, et al. Characterization of the rheological, mucoadhesive, and drug release properties of highly structured gel platforms for intravaginal drug delivery. Biomacromolecules 2009;10:2427-35
38. Bonacucina G, Martelli S, Palmieri GF. Rheological, mucoadhesive and release properties of Carbopol gels in hydrophilic cosolvents. Int J Pharm 2004;282:115-30 (Pubitemid 39178489)
39. Goodwin JW, Hughes RW. Linear Viscoelasticty I. Phenomenological approach. In rheology for chemists: an introduction. Chapter 4 The Royal Society of Chemistry; Cambribge: 2000
40. Ross-Murphy SB. Structure-property relationships in food biopolymer gels and solutions. J Rheology 1995b;36:1451-63
41. Ferry JD. Viscoelastic properties of polymers. John Wiley and Sons; New York: 1980
42. Sahiner N, Singh M, Kee DD, et al. Rheological characterization of a charged cationic hydrogel network across the gelation boundary. Polymer (Guildf) 2006;47:1124-31 (Pubitemid 43199721)
43. Patfoort GA. The stress-strain diagram. In Polymers: an introduction to their physical, mechanical and rheological behaviour. E.Story-Scientia P.V.B.A, Gent; 1999. p. 134-51
44. Lafferty SV, Newton JM, Podczeck F. Characterisation of the mechanical properties of polymer films formed from aqueous polymer dispersions by creep testing. Int J Pharm 2002;239:143-8 (Pubitemid 34615803)
45. Martucci JF, Ruseckaite RA, Vazquez A. Creep of glutaraldehyde- crosslinked gelatin films. Mater Sci Eng 2006;435:681-6 (Pubitemid 44426502)
46. Barry BW. Rheology of pharmaceutical and cosmetic semisolids. Adv Pharm Sci 1974;4:1-72
47. Ceulemans J, Van Santvliet L, Ludwig A. Evaluation of continuous shear and creep rheometry in the physical characterisation of ointments. Int J Pharm 1999;176:187-202 (Pubitemid 29048303)
48. de Paula M, Goissis G, Martins VC. Rheological behavior of anionic collagen injectable gels in the presence of rhamsan for plastic surgery applications. J Mater Sci Mater Med 2007;18:1683-90 (Pubitemid 47222994)
49. Jones DS, Muldoon BC, Woolfson AD, et al. An examination of the rheological and mucoadhesive properties of poly (acrylic acid) organogels designed as platforms for local drug delivery to the oral cavity. J Pharm Sci 2007;96:2632-46 (Pubitemid 47597814)
50. Bercea M, Darie RN, Nita LE, et al. Temperature responsive gels based on Pluronic F127 and poly(vinyl alcohol). Ind Eng Chem Res 2011;50:4199-206
51. Sherman P. Industrial Rheology. Academic Press; New York: 1970
52. Stanley NL, Taylor LJ. Rheological basis of oral characteristics of fluid and semisolid foods: a review. Acta Psychol (Amst) 1993;84:79-92
53. Barreiro-Iglesias R, Alvarez-Lorenzo C, Concheiro A. Incorporation of small quantities of surfactants as a way to improve the rheological and diffusional behavior of carbopol gels. J Control Release 2001;77:59-75 (Pubitemid 33022616)
54. Macosko CW. Rheological principles, Measuremnets and applications. Wiley-vch; New York: 1994
55. Roberts GP, Barnes HA, Carew P. Modelling the flow behaviour of very shear-thinning liquids. Chem Eng Sci 2001;56:5617-23 (Pubitemid 32978626)
56. Perioli L, Ambrogi V, Venezia L, et al. Chitosan and a modified chitosan as agents to improve performances of mucoadhesive vaginal gels. Colloid SurfB Biointerfaces 2008;66:141-5
57. Schott H. Rheology. In: Gennaro AR. editor. Remington's Pharmaceutical Sciences. Mack Publishing Co; Easton, Pennslyvania: 1990. p. 310-26
58. Cross MM. Rheology of non-Newtonian flow: a new flow equation for pseudoplastic systems. J Colloid Sci 1965;20:417-37
59. Crawford RJ. Analysis of polymer melt flow. In plastics engineering. Chapter 5 Butterworth-Heinemann; Oxford: 1998
60. Barnes HA, Hutton JF, Walters K. Viscosity. In: Walters K. editor. An introduction to rheoogy. Chapter 2 Elsevier; Amsterdam: 1989
61. Lenk RS. Polymer Rheology. Applied Science Publishers Ltd; London: 1978
62. Martin A, Swarbrick J, Cammarata A. Rheology. In: Martin A, Swarbrick J, Cammarata A. editor. Physical Pharmacy. Lea & Febiger; Philadelphia: 1987
63. Eadli M, Esmail MN, Vatistas GH. Rheological properties of high concentrations of carboxymethylcellulose solutions. J Appl Polym Sci 2001;79:1787-801 (Pubitemid 32160140)
64. Rayment P, Ross-Murphy SB, Ellis PR. Rheological properties of guar galactomannan and rice starch mixtures. Carbohydr Polym 1995;28:121-30
65. Bird RB, Armstrong RC, Hassanger O. Dynamics of polymeric liquids. In fluid mechanics. John Wiley and Sons; New York: 1987
66. Lapasin R, Lorenzi LD, Pricl S, et al. Flow properties of hydroxypropyl guar gum and its long-chain hydrophobic derivatives. Carbohydr Polym 1995;28:195-202
67. Kieweg S, Katz D. Squeezing flows of vaginal gel formulations relevant to microbicide drug delivery. J Biomech Eng 2006;128:540-53 (Pubitemid 44187314)
68. Owen DH, Peters JJ, Katz DF. Rheological properties of contraceptive gels. Contraception 2000;62:321-6 (Pubitemid 32182420)
69. Barnhart KT, Stolpen A, Pretorius ES, et al. Distribution of a spermicide containing nonoxynol-9 in the vaginal canal and the upper female reproductive tract. Hum Report 2001;16:1151-4 (Pubitemid 32544685)
70. Mauck CK, Katz DF, Sandefer EP, et al. Vaginal distribution of Replens® and K-Y® Jelly using three imaging techniques. Contraception 2008;77:195-204
71. Andrews GP, Gorman SP, Jones DS. Rheological characterisation of primary and binary interactive bioadhesive gels composed of cellulose derivatives designed as ophthalmic viscosurgical devices. Biomaterials 2005;26:571-80 (Pubitemid 38969987)
72. Andrews GP, Jones DS. Rheological characterization of bioadhesive binary polymeric systems designed as platforms for drug delivery implants. Biomacromolecules 2006;7:899-906
73. das Neves J, da Silva MV, Goncalves MP, et al. Rheological properties of vaginal hydrophilic polymer gels. Curr Drug Deliv 2009; 6: 83-92
74. Wille T, Pesun IJ, Combe EC, et al. A clinical pilot study of the time-dependent composition of tooth bleaching systems. J Oral Rehabil 2001;30:510-14 (Pubitemid 37249080)
75. de Paula MR, Goissis G, Martins VC, et al. Injectable gels of anionic collagen: rhamsan composites for plastic correction: preparation, characterization, and rheological properties. J Biomed Mater Res B Appl Biomaterials 2005;75B:393-9 (Pubitemid 41609561)
76. Bonacucina G, Palmieri GF. Acrylic polymers as thickening agents for tetraglycol cosolvent. J Pharm Sci 2006;95:726-36
77. Mahalingam A, Smith E, Fabian J, et al. Design of a semisolid vaginal microbicide gel by relating composition to properties and performance. Pharm Res 2010;27:2478-91