Soluplus®/TPGSGS-based solid dispersions prepared by hot-melt extrusion equipped with twin-screw systems for enhancing oral bioavailability of valsartan

Drug Design, Development and Therapy

Volumn 9, Issue , 2015, Pages 2745-2756

  Lee, Jae Young ^a   Kang, Wie Soo ^b   Piao, Jingpei ^b   Yoon, In Soo ^c   Kim, Dae Duk ^a   Cho, Hyun Jong ^b  

^a Seoul National University   (South Korea)

^b Kangwon National University   (South Korea)

^c Mokpo National University   (South Korea)

Author keywords

Hot melt extrusion; Oral bioavailability; Solid dispersion; Valsartan

Indexed keywords

ALPHA TOCOPHEROL; HYDROCHLORIC ACID; MULTIDRUG RESISTANCE PROTEIN; PHOSPHORIC ACID; POLYMER; TOCOFERSOLAN; VALSARTAN; ANGIOTENSIN 1 RECEPTOR ANTAGONIST; DRUG CARRIER; MACROGOL DERIVATIVE; POLYVINYL CAPROLACTAM-POLYVINYL ACETATE-POLYETHYLENE GLYCOL GRAFT COPOLYMER; POLYVINYL DERIVATIVE;

ANIMAL EXPERIMENT; AREA UNDER THE CURVE; ARTICLE; BLOOD SAMPLING; CENTRIFUGATION; CONTROLLED STUDY; DIFFERENTIAL SCANNING CALORIMETRY; DISPERSION; DRUG ABSORPTION; DRUG ANALYSIS; DRUG BIOAVAILABILITY; DRUG FORMULATION; DRUG MANUFACTURE; DRUG RELEASE; DRUG SCREENING; DRUG SOLUBILITY; ELECTROSPRAY MASS SPECTROMETRY; FLOW RATE; HIGH PERFORMANCE LIQUID CHROMATOGRAPHY; HISTOPATHOLOGY; HOT MELT EXTRUSION; HYDROGEN BOND; IN VITRO STUDY; IN VIVO STUDY; INFRARED SPECTROSCOPY; LETHAL DOSE; LIQUID CHROMATOGRAPHY; MALE; MAXIMUM PLASMA CONCENTRATION; MELTING POINT; MICELLE; MICROCAPSULE; NONHUMAN; RAT; SHEAR STRESS; SOLID STATE; SUPERNATANT; TANDEM MASS SPECTROMETRY; THERMODYNAMICS; TIME TO MAXIMUM PLASMA CONCENTRATION; VISCOSITY; X RAY DIFFRACTION; ANALOGS AND DERIVATIVES; ANIMAL; BIOAVAILABILITY; CHEMISTRY; COMPARATIVE STUDY; MEDICINAL CHEMISTRY; ORAL DRUG ADMINISTRATION; PH; PROCEDURES; SOLUBILITY; SPRAGUE DAWLEY RAT;

ADMINISTRATION, ORAL; ANGIOTENSIN II TYPE 1 RECEPTOR BLOCKERS; ANIMALS; BIOLOGICAL AVAILABILITY; CHEMISTRY, PHARMACEUTICAL; DRUG CARRIERS; DRUG COMPOUNDING; DRUG LIBERATION; HYDROGEN-ION CONCENTRATION; MALE; POLYETHYLENE GLYCOLS; POLYVINYLS; RATS; RATS, SPRAGUE-DAWLEY; SOLUBILITY; VALSARTAN; VITAMIN E;

EID: 84930681473     PISSN: 11778881     EISSN: 11778881     Source Type: Journal    
DOI: 10.2147/DDDT.S84070     Document Type: Article

References (41)

1. Cho HJ, Park JW, Yoon IS, Kim DD. Surface-modified solid lipid nanoparticles for oral delivery of docetaxel: enhanced intestinal absorption and lymphatic uptake. Int J Nanomedicine. 2014;9:495–504.
2. Kim JE, Yoon IS, Cho HJ, Kim DH, Choi YH, Kim DD. Emulsion-based colloidal nanosystems for oral delivery of doxorubicin: improved intestinal paracellular absorption and alleviated cardiotoxicity. Int J Pharm. 2014;464(1–2):117–126.
3. Yin YM, Cui FD, Mu CF, et al. Docetaxel microemulsion for enhanced oral bioavailability: preparation and in vitro and in vivo evaluation. J Control Release. 2009;140(2):86–94.
4. Baek HH, Kim DH, Kwon SY, et al. Development of novel ibuprofen-loaded solid dispersion with enhanced bioavailability using cycloamylose. Arch Pharm Res. 2012;35(4):683–689.
5. Kim SA, Kim SW, Choi HK, Han HK. Enhanced systemic exposure of saquinavir via the concomitant use of curcumin-loaded solid dispersion in rats. Int J Pharm. 2013;49(5):800–804.
6. Alam MA, Ali R, Al-Jenoobi FI, Al-Mohizea AM. Solid dispersions: a strategy for poorly aqueous soluble drugs and technology updates. Expert Opin Drug Deliv. 2012;9(11):1419–1440.
7. Lakshman JP, Cao Y, Kowalski J, Serajuddin AT. Application of melt extrusion in the development of a physically and chemically stable high-energy amorphous solid dispersion of a poorly water-soluble drug. Mol Pharm. 2008;5(6):994–1002.
8. Djuris J, Nikolakakis I, Ibric S, Djuric Z, Kachrimanis K. Preparation of carbamazepine-Soluplus solid dispersions by hot-melt extrusion, and prediction of drug-polymer miscibility by thermodynamic model fitting. Eur J Pharm Biopharm. 2013;84(1):228–237.
9. Leuner C, Dressman J. Improving drug solubility for oral delivery using solid dispersions. Eur J Pharm Biopharm. 2000;50(1):47–60.
10. Guo Z, Lu M, Li Y, et al. The utilization of drug-polymer interactions for improving the chemical stability of hot-melt extruded solid dispersions. J Pharm Pharmcol. 2014;66(2):285–296.
11. Linn M, Collnot EM, Djuric D, et al. Soluplus® as an effective absorption enhancer of poorly soluble drugs in vitro and in vivo. Eur J Pharm Sci. 2012;45(3):336–343.
12. Shin SC, Kim J. Physicochemical characterization of solid dispersion of furosemide with TPGS. Int J Pharm. 2003;251(1–2):79–84.
13. Van Eerdenbrugh B, Van Speybroeck M, Mols R, et al. Itraconazole/TPGS/Aerosil200 solid dispersions: characterization, physical stability and in vivo performance. Eur J Pharm Sci. 2009;38(3):270–278.
14. Cao QR, Liu Y, Xu WJ, Lee BJ, Yang M, Cui JH. Enhanced oral bioavailability of novel mucoadhesive pellets containing valsartan prepared by a dry powder-coating technique. Int J Pharm. 2012;434(1–2):325–333.
15. Beg S, Swain S, Singh HP, Patra ChN, Rao ME. Development, optimization, and characterization of solid self-nanoemulsifying drug delivery systems of valsartan using porous carriers. AAPS Pharm Sci Tech. 2012;13(4):1416–1427.
16. Li DX, Yan YD, Oh DH, et al. Development of valsartan-loaded gelatin microcapsule without crystal change using hydroxypropylmethylcellulose as a stabilizer. Drug Deliv. 2010;17(5):322–329.
17. Yan YD, Sung JH, Kim KK, et al. Novel valsartan-loaded solid dispersion with enhanced bioavailability and no crystalline changes. Int J Pharm. 2012;422(1–2):202–210.
18. Crowley MM, Zhang F, Repka MA, et al. Pharmaceutical applications of hot-melt extrusion: part I. Drug Dev Ind Pharm. 2007;33(9):909–926.
19. Aharoni SM. Increased glass transition temperature in motionally constrained semicrystalline polymers. Polym Adv Technol. 1998;9(3):169–201.
20. Nakamichi K, Nakano T, Yasuura H, Izumi S, Kawashima Y. The role of the kneading paddle and the effects of screw revolution speed and water content on the preparation of solid dispersions using a twin-screw extruder. Int J Pharm. 2002;241(2):203–211.
21. Tran TT, Tran PH, Park JB, Lee BJ. Effects of solvents and crystallization conditions on the polymorphic behaviors and dissolution rates of valsartan. Arch Pharm Res. 2012;35(7):1223–1230.
22. Hughey JR, Keen JM, Miller DA, Kolter K, Langley N, McGinity JW. The use of inorganic salts to improve the dissolution characteristics of tablets containing Soluplus®-based solid dispersions. Eur J Pharm Sci. 2013;48(4–5):758–766.
23. Mu L, Feng SS. A novel controlled release formulation for the anticancer drug paclitaxel (Taxol): PLGA nanoparticles containing vitamin E TPGS. J Control Release. 2003;86(1):33–48.
24. Bhugra C, Pikal MJ. Role of thermodynamic, molecular, and kinetic factors in crystallization from the amorphous state. J Pharm Sci. 2008;97(4):1329–1349.
25. Yu L. Amorphous pharmaceutical solids: preparation, characterization and stabilization. Adv Drug Deliv Rev. 2001;48(1):27–42.
26. Flesch G, Muller P, Lloyd P. Absolute bioavailability and pharmacokinetics of valsartan, an angiotensin II receptor antagonist, in man. Eur J Clin Pharmacol. 1997;52(2):115–120.
27. Pina MF, Zhao M, Pinto JF, Sousa JJ, Craig DQ. The influence of drug physical state on the dissolution enhancement of solid dispersions prepared via hot-melt extrusion: a case study using olanzapine. J Pharm Sci. 2014;103(4):1214–1223.
28. Chen W, Miao YQ, Fan DJ, et al. Bioavailability study of berberine and the enhancing effects of TPGS on intestinal absorption in rats. AAPS Pharm Sci Tech. 2011;12(2):705–711.
29. Cho HJ, Balakrishnan P, Chung SJ, Shim CK, Kim DD. Evaluation of protein stability and in vitro permeation of lyophilized polysaccharides-based microparticles for intranasal protein delivery. Int J Pharm. 2011;416(1):77–84.
30. Guo Y, Luo J, Tan S, Otieno BO, Zhang Z. The applications of vitamin E TPGS in drug delivery. Eur J Pharm Sci. 2013;49(2):175–186.
31. Varma MV, Panchagnula R. Enhanced oral paclitaxel absorption with vitamin E-TPGS: effect on solubility and permeability in vitro, in situ and in vivo. Eur J Pharm Sci. 2005;25(4–5):445–453.
32. Challa VR, Babu PR, Challa SR, Johnson B, Maheswari C. Pharmacokinetic interaction study between quercetin and valsartan in rats and in vitro models. Drug Dev Ind Pharm. 2013;39(6):865–872.
33. Lin X, Skolnik S, Chen X, Wang J. Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model. Drug Metab Dispos. 2011;39(2):265–274.
34. Zhang Z, Tan S, Feng SS. Vitamin E TPGS as a molecular biomaterial for drug delivery. Biomaterials. 2012;33(19):4889–4906.
35. Poudel BK, Marasini N, Tran TH, Choi HG, Yong CS, Kim JO. Formulation, characterization and optimization of valsartan self-microemulsifying drug delivery system using statistical design of experiment. Chem Pharm Bull. 2012;60(11):1409–1418.
36. Singh SK, Vuddanda PR, Singh S, Srivastava AK. A comparison between use of spray and freeze drying techniques for preparation of solid self-microemulsifying formulation of valsartan and in vitro and in vivo evaluation. Biomed Res Int. 2013;2013:909045.
37. Zhang Y, Che E, Zhang M, et al. Increasing the dissolution rate and oral bioavailability of the poorly water-soluble drug valsartan using novel hierarchical porous carbon monoliths. Int J Pharm. 2014;473(1–2):375–383.
38. Kim MS, Baek IH. Fabrication and evaluation of valsartan-polymer- surfactant composite nanoparticles by using the supercritical antisolvent process. Int J Nanomedicine. 2014;9:5167–5176.
39. Ma Q, Sun H, Che E, et al. Uniform nano-sized valsartan for dissolution and bioavailability enhancement: influence of particle size and crystalline state. Int J Pharm. 2013;441(1–2):75–81.
40. Sokol RJ, Heubi JE, Butler-Simon N, McClung HJ, Lilly JR, Silverman A. Treatment of vitamin E deficiency during chronic childhood cholestasis with oral d-alpha-tocopheryl polyethylene glycol-1000 succinate. Gastroenterology. 1987;93(5):975–985.
41. Constantinides PP, Han J, Davis SS. Advances in the use of tocols as drug delivery vehicles. Pharm Res. 2006;23(2):243–255.