Application of model-based methods to characterize exenatide-loaded double-walled microspheres: In vivo release, pharmacokinetic/pharmacodynamic model, and in vitro and in vivo correlation

Journal of Pharmaceutical Sciences

Volumn 101, Issue 10, 2012, Pages 3946-3961

  Li, Xingang ^a   Li, Liang ^a   Wang, Xipei ^a   Ren, Yupeng ^a   Zhou, Tianyan ^a   Lu, Wei ^a  

^a PEKING UNIVERSITY   (China)

Author keywords

Controlled release; Dose response; Double walled microspheres; Exenatide; In vitro and in vivo correlation; Pharmacokinetic pharmacodynamic model; Simulation; Transit compartment model

Indexed keywords

EXENDIN 4; INSULIN; MICROSPHERE;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; ANTIDIABETIC ACTIVITY; ARTICLE; CONTROLLED STUDY; CORRELATIONAL STUDY; DIABETES MELLITUS; DRUG DEGRADATION; DRUG DELIVERY SYSTEM; DRUG RELEASE; EXPERIMENTAL DIABETES MELLITUS; IN VITRO STUDY; IN VIVO STUDY; INSULIN LIKE ACTIVITY; MALE; NONHUMAN; PHARMACODYNAMICS; PHYSICAL CHEMISTRY; RAT; SIMULATION; SINGLE DRUG DOSE;

EID: 84865359777     PISSN: 00223549     EISSN: 15206017     Source Type: Journal    
DOI: 10.1002/jps.23236     Document Type: Article

References (44)

1. Parkes DG, Nielsen LL, Young AA. 2004. Pharmacology of exenatide (synthetic exendin-4): A potential therapeutic for improved glycemic control of type 2 diabetes. Regul Pept 117:77-88.
2. Young AA, Gedulin BR, Bhavsar S, Bodkin N, Jodka C, Hansen B, Denaro M. 1999. Glucose-lowering and insulin-sensitizing actions of exendin-4 - Studies in obese diabetic (ob/ob, db/db) mice, diabetic fatty Zucker rats, and diabetic rhesus monkeys (Macaca mulatta). Diabetes 48:1026-1034.
3. Kolterman OG, Kim DD, Shen L, Ruggles JA, Nielsen LL, Fineman MS, Baron AD. 2005. Pharmacokinetics, pharmacodynamics, and safety of exenatide in patients with type 2 diabetes mellitus. Am J Health Syst Pharm 62:173-181.
4. Parkes DG, Pittner R, Jodka C, Smith P, Young A. 2001. Insulinotropic actions of exendin-4 and glucagon-like peptide-1 in vivo and in vitro. Metabolism 50:583-589.
5. Krentz AJ, Patel MB, Bailey CJ. 2008. New drugs for type 2 diabetes mellitus: What is their place in therapy? Drugs 68:2131-2162.
6. Wright SG, Christenson T, Yeah TY, Rickey ME, Hotz JM, Kumar R, Costantino HR. 2008. Polymer-based sustained release device. Patent US7456254B2.
7. Kwak HH, Shim WS, Hwang S, Son MK, Kim YJ, Kim TH, Yoon ZH, Youn HJ, Lee GI, Kang SH, Shim CK. 2009. Pharmacokinetics and efficacy of a biweekly dosage formulation of exenatide in Zucker diabetic fatty (ZDF) rats. Pharm Res 26:2504-2512.
8. Yang HJ, Park IS, Na K. 2009. Biocompatible microspheres based on acetylated polysaccharide prepared from water-in-oil-in-water (W1/O/W2) double-emulsion method for delivery of type II diabetic drug (exenatide). Colloids Surf A Physicochem Eng Aspects 340:115-120.
9. Chen Y, Liu B, Dong QG, Wang MS, Shi L, Wu YG, Yu XH, Shi YY, Shan YM, Jiang CL, Zhang XZ, Gu TJ, Kong W. 2010. Preparation, characterization, and pharmacodynamics of exenatide-loaded poly(dl-lactic-co-glycolic acid) microspheres. Chem Pharm Bull 58:1474-1479.
10. Pekarek KJ, Jacob JS, Mathiowitz E. 1994. Double-walled polymer microspheres for controlled drug-release. Nature 367:258-260.
11. Zheng W. 2009. A water-in-oil-in-oil-in-water (W/O/O/W) method for producing drug-releasing, double-walled microspheres. Int J Pharm 374:90-95.
12. Tan EC, Lin R, Wang CH. 2005. Fabrication of double-walled microspheres for the sustained release of doxorubicin. J Colloid Interface Sci 291:135-143.
13. Berkland C, Cox A, Kim K, Pack DW. 2004. Three-month, zero-order piroxicam release from monodispersed double-walled microspheres of controlled shell thickness. J Biomed Mater Res A 70:576-584.
14. Pollauf EJ, Berkland C, Kim KK, Pack DW. 2005. In vitro degradation of polyanhydride/polyester core-shell double-wall microspheres. Int J Pharm 301:294-303.
15. Mathiowitz E, Leach KJP. 1998. Degradation of double-walled polymer microspheres of PLLA and P(CPP: SA)20: 80. I. In vitro degradation. Biomaterials 19:1973-1980.
16. Mathiowitz E, Leach KJP, Takahashi S. 1998. Degradation of double-walled polymer microspheres of PLLA and P(CPP: SA)20: 80. II. in vivo degradation. Biomaterials 19:1981-1988.
17. Savic RM, Jonker DM, Kerbusch T, Karlsson MO. 2007. Implementation of a transit compartment model for describing drug absorption in pharmacokinetic studies. J Pharmacokinet Pharmacodyn 34:711-726.
18. Kagan L, Hoffman A. 2008. Selection of drug candidates for gastroretentive dosage forms: Pharmacokinetics following continuous intragastric mode of administration in a rat model. Eur J Pharm Biopharm 69:238-246.
19. Lehto P, Kortejarvi H, Liimatainen A, Ojala K, Kangas H, Hirvonen J, Tanninen VP, Peltonen L. 2011. Use of conventional surfactant media as surrogates for FaSSIF in simulating in vivo dissolution of BCS class II drugs. Eur J Pharm Biopharm 78:531-538.
20. Sun YN, Jusko WJ. 1998. Transit compartments versus gamma distribution function to model signal transduction processes in pharmacodynamics. J Pharm Sci 87:732-737.
21. Hamberg AK, Dahl ML, Barban M, Scordo MG, Wadelius M, Pengo V, Padrini R, Jonsson EN. 2007. A PK-PD model for predicting the impact of age, CYP2C9, and VKORC1 genotype on individualization of warfarin therapy. Clin Pharmacol Ther 81:529-538.
22. Li L, Li ZQ, Deng CH, Ning MR, Li HQ, Bi SS, Zhou TY, Lu W. 2012. A mechanism-based pharmacokinetic/pharmacodynamic model for CYP3A1/2 induction by dexamethasone in rats. Acta Pharmacol Sin 33:127-136.
23. Jiang W, Kim S, Zhang X, Lionberger RA, Davit BM, Conner DP, Yu LX. 2011. The role of predictive biopharmaceutical modeling and simulation in drug development and regulatory evaluation. Int J Pharm 418:151-160.
24. Landersdorfer CB, Jusko WJ. 2008. Pharmacokinetic/pharmacodynamic modelling in diabetes mellitus. Clin Pharmacokinet 47:417-448.
25. Silber HE, Jauslin PM, Frey N, Karlsson MO. 2010. An integrated model for the glucose-insulin system. Basic Clin Pharmacol Toxicol 106:189-194.
26. Amidi M, Krudys KM, Snel CJ, Crommelin DJ, Della Pasqua OE, Hennink WE, Jiskoot W. 2008. Efficacy of pulmonary insulin delivery in diabetic rats: Use of a model-based approach in the evaluation of insulin powder formulations. J Control Release 127:257-266.
27. Ryan SM, Frias JM, Wang X, Sayers CT, Haddleton DM, Brayden DJ. 2011. PK/PD modelling of comb-shaped PEGylated salmon calcitonin conjugates of differing molecular weights. J Control Release 149:126-132.
28. Ackaert OW, De Graan J, Capancioni R, Della Pasqua OE, Dijkstra D, Westerink BH, Danhof M, Bouwstra JA. 2010. The in vitro and in vivo evaluation of new synthesized prodrugs of 5-OH-DPAT for iontophoretic delivery. J Control Release 144:296-305.
29. Sun Y, Wang J, Zhang X, Zhang Z, Zheng Y, Chen D, Zhang Q. 2008. Synchronic release of two hormonal contraceptives for about one month from the PLGA microspheres: In vitro and in vivo studies. J Control Release 129:192-199.
30. Jantratid E, De Maio V, Ronda E, Mattavelli V, Vertzoni M, Dressman JB. 2009. Application of biorelevant dissolution tests to the prediction of in vivo performance of diclofenac sodium from an oral modified-release pellet dosage form. Eur J Pharm Sci 37:434-441.
31. Zolnik BS, Burgess DJ. 2008. Evaluation of in vivo-in vitro release of dexamethasone from PLGA microspheres. J Control Release 127:137-145.
32. Buchwald P. 2003. Direct, differential-equation-based in-vitro-in-vivo correlation (IVIVC) method. J Pharm Pharmacol 55:495-504.
33. Sah H. 1997. A new strategy to determine the actual protein content of poly(lactide-co-glycolide) microspheres. J Pharm Sci 86:1315-1318.
34. Reed MJ, Meszaros K, Entes LJ, Claypool MD, Pinkett JG, Gadbois TM, Reaven GM. 2000. A new rat model of type 2 diabetes: The fat-fed, streptozotocin-treated rat. Metabolism 49:1390-1394.
35. Li XG, Li L, Zhou X, Chen Y, Ren YP, Zhou TY, Lu W. 2012. Pharmacokinetic/pharmacodynamic studies on exenatide in diabetic rats. Acta Pharmacol Sin (In press).
36. Balan G, Timmins P, Greene DS, Marathe PH. 2001. In vitro-in vivo correlation (IVIVC) models for metformin after administration of modified-release (MR) oral dosage forms to healthy human volunteers. J Pharm Sci 90:1176-1185.
37. Burgess DJ, Hussain AS, Ingallinera TS, Chen ML. 2002. Assuring quality and performance of sustained and controlled release parenterals: Workshop report. AAPS PharmSci 4:E7.
38. Kokai LE, Tan H, Jhunjhunwala S, Little SR, Frank JW, Marra KG. 2010. Protein bioactivity and polymer orientation is affected by stabilizer incorporation for double-walled microspheres. J Control Release 141:168-176.
39. Rahman NA, Mathiowitz E. 2004. Localization of bovine serum albumin in double-walled microspheres. J Control Release 94:163-175.
40. Spenlehauer G, Vert M, Benoit JP, Boddaert A. 1989. In vitro and in vivo degradation of poly(d, l lactide/glycolide) type microspheres made by solvent evaporation method. Biomaterials 10:557-563.
41. Tracy MA, Ward KL, Firouzabadian L, Wang Y, Dong N, Qian R, Zhang Y. 1999. Factors affecting the degradation rate of poly(lactide-co-glycolide) microspheres in vivo and in vitro. Biomaterials 20:1057-1062.
42. Jiang G, Woo BH, Kang F, Singh J, DeLuca PP. 2002. Assessment of protein release kinetics, stability and protein polymer interaction of lysozyme encapsulated poly(d, l-lactide-co-glycolide) microspheres. J Control Release 79:137-145.
43. Jiang G, Qiu W, DeLuca PP. 2003. Preparation and in vitro/in vivo evaluation of insulin-loaded poly(acryloyl-hydroxyethyl starch)-PLGA composite microspheres. Pharm Res 20:452-459.
44. Machida Y, Onishi H, Kurita A, Hata H, Morikawa A. 2000. Pharmacokinetics of prolonged-release CPT-11-loaded microspheres in rats. J Control Release 66:159-175.