Docetaxel-loaded thermosensitive liquid suppository: optimization of rheological properties

다국어 초록 (Multilingual Abstract)

The main purpose of this work was to optimizethe rheological properties of docetaxel (DCT)-loadedthermosensitive liquid suppositories for rectal administration.
DCT-loaded liquid suppositories were prepared by acold method and characterized in terms of physicochemicaland viscoelastic properties. Major formulation parametersincluding poloxamer (P407) and Tween 80 were optimizedto adjust the thermogelling and mucoadhesive propertiesfor rectal administration. Notably, the gel strength andmucoadhesive force significantly increased with theincrease in these variables. Furthermore, DCT incorporationdid not alter the viscoelastic behavior, and the meanparticle size of nanomicelles in it was approximately16 nm with a distinct spherical shape. The formulationexisted as liquid at room temperature and transformed intogel at physiological temperature through the reverse gelationphenomenon. Thus, DCT-loaded thermosensitiveliquid suppositories [DCT/P407/P188/Tween 80 (0.25/11/15/10 %)] with optimal gel properties were easy to prepareand administer rectally, and might enable the gel to stay inthe rectum without getting out from rectum.

참고문헌 (Reference)

1 Yuan, Y., "Thermosensitive and mucoadhesive in situ gel based on poloxamer as new carrier for rectal administration of nimesulide" 430 : 114-119, 2012

2 Du, W., "Synthesis and evaluation of water-soluble docetaxel prodrugsdocetaxel esters of malic acid" 15 : 6323-6330, 2007

3 Jun, Y. J, "Stable and efficient delivery of docetaxel by micelleencapsulation using a tripodal cyclotriphosphazene amphiphile" 422 : 374-380, 2012

4 Elsabahy, M., "Solubilization of docetaxel in poly(ethylene oxide)-blockpoly(butylene/styrene oxide)micelles" 8 : 2250-2257, 2007

5 Xuan, J. J., "Rheological characterization and in vivo evaluation of thermosensitive poloxamer-based hydrogel for intramuscular injection of piroxicam" 395 : 317-323, 2010

6 Chen, J., "Preparation, characterization and in vitro evaluation of solid dispersions containing docetaxel" 34 : 588-594, 2008

7 Straubinger, R. M., "Preparation and characterization of taxane-containing liposomes" 391 : 97-117, 2005

8 Gao, K., "Preparation and characterization of a submicron lipid emulsion of docetaxel, submicron lipid emulsion of docetaxel" 34 : 1227-1237, 2008

9 Wils, P., "Polarized transport of docetaxel and vinblstine mediated by P-glycoprotein in human intestinal epithelial cell monolayers" 48 : 1528-1530, 1994

10 Sambuelli, A. M., "Multidrug resistance gene(MDR-1)expression in the colonic mucosa of patients with refractory ulcerative colitis" 36 : 23-32, 2006

11 Mayol, L., "Injectable thermally responsive mucoadhesive gel for sustained protein delivery" 12 : 28-33, 2011

12 Engels, F. K., "Influence of high-dose ketoconazole on the pharmacokinetics of docetaxel" 5 : 833-839, 2006

13 Sakai, M., "Increased bioavailability of tacrolimus after rectal administration in rats" 27 : 1480-1482, 2004

14 Ryu, J. M., "Increased bioavailability of propranolol in rats by retaining thermally gelling liquid suppositories in the rectum" 59 : 163-172, 1999

15 Barakat, N. S, "In vitro and in vivo characteristics of a thermogelling rectal delivery system of etodolac" 10 : 724-731, 2009

16 Klueglich, M., "Ibuprofen Extrudate, a Novel, Rapidly Dissolving Ibuprofen Formulation, Relative Bioavailability Compared to Ibuprofen Lysinate and Regular Ibuprofen, and Food Effect on All Formulations" 45 : 1055-1061, 2005

17 Yong, C. S., "Enhanced rectal bioavailability of ibuprofen in rats by poloxamer 188 and menthol" 269 : 169-176, 2004

18 Yan, Y. D., "Enhanced oral bioavailability of docetaxel in rats by four consecutive days of pre-treatment with curcumin" 399 : 116-120, 2010

19 Hu, K., "Enhanced oral bioavailability of docetaxel by lecithin nanoparticles, preparation, in vitro, and in vivo evaluation" 7 : 3537-3545, 2012

20 Yong, C. S., "Effect of sodium chloride on the gelation temperature, gel strength and bioadhesive force of poloxamer gels containing diclofenac sodium" 226 : 195-205, 2001

21 Choi, H. G., "Effect of additives on the physicochemical properties of liquid suppository" 190 : 13-19, 1999

22 Kintzel, P. E., "Docetaxelassociated epiphora" 26 : 853-867, 2006

23 Seo, Y. G., "Docetaxel-loaded thermosensitive and bioadhesive nanomicelles as a rectal drug delivery system for enhanced chemotherapeutic effect" 30 (30): 1860-1870, 2013

24 Esmaeili, F., "Docetaxel-albumin conjugates, preparation, in vitro evaluation and biodistribution studies" 98 : 2718-2730, 2009

25 Yin, Y. M., "Docetaxel microemulsion for enhanced oral bioavailability, preparation and in vitro and in vivo evaluation" 140 : 86-94, 2009

26 Choi, H. G., "Development of in situ-gelling and mucoadhesive acetaminophen liquid suppository" 165 : 33-44, 1998

27 Wang, L., "Design and optimization of a new self-nanoemulsifying drug delivery system" 330 : 443-448, 2009

28 Zrieki, A., "Cyclooxygenase-2 inhibitors prevent trinitrobenzene sulfonic acid-induced P-glycoprotein up-regulation in vitro and in vivo" 636 : 189-197, 2010

29 Veyries, M. L., "Controlled release of vancomycin from poloxamer 407 gels" 192 : 183-193, 1999

30 Malingre, M. M., "Coadministration of cyclosporine strongly enhances the oral bioavailability of docetaxel" 19 : 1160-1166, 2001

31 Esmaeili, F., "Cellular cytotoxicity and in vivo biodistribution of docetaxel poly(lactide-co-glycolide)nanoparticles" 21 : 43-52, 2010

32 Young Keun Choi, "Biostable Poly(ethylene oxide)-b-poly(methacrylic acid) Micelles forpH-triggered Release of Doxorubicin" 한국약제학회 41 (41): 111-115, 2011

33 Ben Reguiga, M., "Bioavailability and tissular distribution of docetaxel, a P-glycoprotein substrate, are modified by interferon-alpha in rats" 59 : 401-408, 2007

34 Yang, Y., "A novel mixed micelle gel with thermo-sensitive property for the local delivery of docetaxel" 135 : 175-182, 2009