Effect of agitation regimen on the in vitro release of leuprolide from poly(lactic-co-glycolic) acid microparticles

Journal of Pharmaceutical Sciences

Volumn 101, Issue 3, 2012, Pages 1212-1220

  Schoubben, Aurélie ^a   Blasi, Paolo ^a   Deluca, Patrick P ^b  

^a UNIVERSITY OF PERUGIA   (Italy)

^b UNIVERSITY OF KENTUCKY   (United States)

Author keywords

Agitation regimen; Controlled release delivery; In vitro release; Koizumi equation; Leuprolide acetate; Microencapsulation; Molecular weight determination; Peptide delivery; PLGA microparticles; Polymer biodegradation

Indexed keywords

LEUPRORELIN; PEPTIDE; PHOSPHATE BUFFERED SALINE; POLYESTER; POLYLACTIC ACID; POLYMER; RESOMER;

AGITATION; ARTICLE; DRUG RELEASE; ENCAPSULATION; HYDRATION; IN VITRO STUDY; MOLECULAR WEIGHT; PARTICLE SIZE; REPRODUCIBILITY;

EID: 84855872350     PISSN: 00223549     EISSN: 15206017     Source Type: Journal    
DOI: 10.1002/jps.23029     Document Type: Article

References (54)

1. Rathbone MJ, Hadgraft J, Roberts MS. 2003. Modified-release drug delivery technology. New York: Marcel Dekker.
2. Chaubal M. 2002. Polylactides/glycolides-excipients for injectable drug delivery and beyond. Drug Deliv Technol 5:34-36.
3. Frazza EJ, Schmitt EE. 1971. A new absorbable suture. Biomed Mater Res 5:43-58.
4. Woo BH, Kostanski JW, Gebrekidan S, Dani BA, Thanoo BC, DeLuca PP. 2001. Preparation, characterization and in vivo evaluation of 120-day poly(d, l-lactide) leuprolide microsphere. J Control Release 75:307-315.
5. Okada H. 1997. One- and three-month release injectable microspheres of the LH-RH superagonist leuprorelin acetate. Adv Drug Deliv Rev 28:43-70.
6. D'Souza SS, DeLuca PP. 2006. Methods to assess in vitro drug release from injectable polymeric particulate systems. Pharm Res 23:460-474.
7. Trachtenberg J. 1983. The treatment of metastatic prostatic cancer with a potent luteinizing hormone releasing hormone analogue. J Urol 129:1149-1152.
8. Wojciechowski NJ. 1986. Leuprolide: A gonadotropin-releasing hormone analogue for the palliative treatment of prostatic cancer. Drug Intell Clin Pharm 20:746-751.
9. Li WI, Anderson KW, DeLuca PP. 1995. Kinetic and thermodynamic modelling of the formation of polymeric microspheres using solvent extraction/evaporation method. J Control Release 37:187-198.
10. Li WI, Anderson KW, Mehta RC, DeLuca PP. 1995. Prediction of solvent removal profile and effect on properties for peptide-loaded PLGA microspheres prepared by solvent extraction/evaporation method. J Control Release 37:199-214.
11. Jeyanthi R, Mehta RC, Thanoo BC, DeLuca PP. 1997. Effect of processing parameters on the properties of peptide-containing PLGA microspheres. J Microencapsul 14:163-174.
12. Yang YY, Chung TS, Bai XL, Chan WK. 2000. Effect of preparation conditions on morphology and release profiles of biodegradable polymeric microspheres containing protein fabricated by double-emulsion method. Chem Eng Sci 55:2223-2236.
13. Yi-Yan Y, Hui-Hui C, Tai-Shung C. 2000. Effect of preparation temperature on the characteristics and release profiles of PLGA microspheres containing protein fabricated by double-emulsion solvent extraction/evaporation method. J Control Release 69:81-96.
14. Yi-Yan Y, Tai-Shung C, Ngee Ping N. 2001. Morphology, drug distribution, and in vitro release profiles of biodegradable polymeric microspheres containing protein fabricated by double-emulsion solvent extraction/evaporation method. Biomaterials 22:231-341.
15. Pillay V, Fassihi R. 1999. Unconventional dissolution methodologies. J Pharm Sci 88:843-851.
16. Siewert M, Dressman J, Brown CK, Shah VP. 2003. FIP/AAPS guidelines to dissolution/in vitro release testing of novel/special dosage forms. AAPS PharmSciTech 4(1):43-52.
17. Azarmi S, Roa W, Löbenberg R. 2007. Current perspectives in dissolution testing of conventional and novel dosage forms. Int J Pharm 328:12-21.
18. Batycky RP, Hanes J, Langer R, Edwards DA. 1997. A theoretical model of erosion and macromolecular drug release from biodegrading microspheres. J Pharm Sci 86:1464-1477.
19. Li S. 1999. Hydrolytic degradation characteristics of aliphatic polyesters derived from lactic and glycolic acids. J Biomed Mater Res Appl Biomater 48:342-353.
20. Li SM, Garreau H, Vert M. 1990. Structure-property relationships in the case of the degradation of massive aliphatic poly-(α-hydroxy acids) in aqueous media, part 1. J Mater Sci Mater Med 1:123-130.
21. Brunner A, Mäder K, Göpferich A. 1999. pH and osmotic pressure inside biobegradable microspheres during erosion. Pharm Res 16:847-853.
22. Fu K, Pack DW, Klibanov AM, Langer R. 2000. Visual evidence of acidic environment within degrading poly(lactic-co-glycolic acid) (PLGA) microspheres. Pharm Res 17:100-106.
23. Ding AG, Shenderova A, Schwendeman SP. 2006. Prediction of microclimate pH in poly(lactic-co-glycolic acid) film. J Am Chem Soc 128:5384-5390.
24. Blanco-Prìeto MJ, Besseghir K, Orsolini P, Heimgartner F, Deuschel C, Merkle HP, Nam-Trân H, Gander B. 1999. Importance of the test medium for the release kinetics of a somatostatin analogue from poly(d, l-lactide-co-glycolide) microspheres. Int J Pharm 184:243-250.
25. Dunne M, Corrigan OI, Ramtoola Z. 2000. Influence of particle size and dissolution conditions on the degradation properties of polylactide-co-glycolide particles. Biomaterials 21:1659-1668.
26. Faisant N, Akiki J, Siepmann F, Benoit JP, Siepmann J. 2006. Effects of the type of release medium on drug release from PLGA-based microparticles: Experiment and theory. Int J Pharm 314:189-197.
27. Shameem M, Lee H, DeLuca PP. 1999. A short term (accelerated release) approach to evaluate peptide release from PLGA depot-formulations. AAPS Pharm Sci 1(3):1-6.
28. Bain DF, Munday DL, Smith A. 1999. Modulation of rifampicin release from spray-dried microspheres using combinations of poly-(d, l-lactide). J Microencapsul 16:369-385.
29. Hayes S, Dunne A, Smart T, Davis J. 2004. Interpretation and optimization of the dissolution specifications for a modified release product with an in vivo-in vitro correlation (IVIVC). J Pharm Sci 93:571-581.
30. Zolnik BS, Raton JL, Burgess DJ. 2005. Application of USP apparatus 4 and in situ fiber optic analysis to microsphere release testing. Dissolution Technol 12(2):11-14.
31. Marques MRC, Loebenberg R, Almukainzi M. 2011. Simulated biological fluids with possible application in dissolution testing. Dissolution Technol 18(3):15-28.
32. Klose D, Siepmann F, Willart JF, Descamps M, Siepmann J. 2010. Drug release from PLGA-based microparticles: Effects of the "microparticle:bulk fluid" ratio. Int J Pharm 383:123-131.
33. Klose D, Delplace C, Siepmann J. 2011. Unintended potential impact of perfect sink conditions on PLGA degradation in microparticles. Int J Pharm 404:75-82.
34. Rawat A, Stippler E, Shah VP, Burgess DJ. 2011. Validation of USP apparatus 4 method for microsphere in vitro release testing using Risperdal® Consta®. Int J Pharm 420:198-205.
35. D'Souza SS, Faraj JA, DeLuca PP. 2005. A model-dependent approach to correlate accelerated with real-time release from biodegradable microspheres. AAPS Pharm Sci Tech 6(4):E553-E564.
36. Koizumi T, Panomsuk SP. 1995. Release of medicaments from spherical matrices containing drug in suspension: Theoretical aspects. Int J Pharm 116:45-49.
37. Kanjickal DG, Lopina ST. 2004. Modeling of drug release from polymeric delivery systems-A review. Crit Rev Ther Drug Carrier Syst 21:345-386.
38. Faisant N, Siepmann J, Benoît JP. 2002. PLGA-based microparticles: Elucidation of mechanisms and a new, simple mathematical model quantifying drug release. Eur J Pharm Sci 15:355-366.
39. Siepmann J, Faisant N, Akiki J, Richard J, Benoît JP. 2004. Effect of size of biodegradable microparticles on drug release: Experiment and theory. J Control Release 96:123-134.
40. Moore JW, Flanner HH. 1996. Mathematical comparison of curves with an emphasis on in vitro dissolution profiles. Pharm Tech 20:64-74.
41. Shah VP, Tsong Y, Sathe P, Liu JP. 1998. In vitro dissolution profile comparison-Statistics and analysis of the similarity factor, f2. Pharm Res 15:889-896.
42. Ma M, Lin R, Liu J. 1999. Statistical evaluations of dissolution similarity. Stat Sin 9:1011-1027.
43. US Pharmacopeia. General chapters 1088, in vitro and in vivo evaluation of dosage forms, and 1090, dissolution and in vitro product performance.
44. Allison SD. 2008. Analysis of initial burst in PLGA microparticles. Expert Opin Drug Deliv 5:615-628.
45. Frank A, Rath SK, Boey F, Venkatraman S. 2004. Study of the initial stages of drug release from a degradable matrix of poly(d, l-lactide-co-glycolide). Biomaterials 25:813-821.
46. 31P NMR spectroscopy. Proc Int Symp Control Release Bioact Mater 23:133-134.
47. Grizzi I, Garreau H, Li S, Vert M. 1995. Hydrolytic degradation of devices based on poly(dl-lactic acid) size-dependence. Biomaterials 16:305-311.
48. Park TG. 1995. Degradation of poly(lactic-co-glycolic acid) microspheres: Effect of copolymer composition. Biomaterials 16:1123-1130.
49. Blasi P, D'Souza SS, Selmin F, DeLuca PP. 2005. Plasticizing effect of water on poly(lactide-co-glycolide). J Control Release 108:1-9.
50. Passerini N, Craig DQM. 2001. An investigation into the effects of residual water on the glass transition temperature of polylactide microspheres using modulated temperature DSC. J Control Release 73:111-115.
51. Fredenberg S, Reslow M, Axelsson A. 2005. Measurement of protein diffusion through poly(d, l-lactide-co-glycolide). Pharm Dev Technol 10:299-307.
52. Liu WG, De Yao K. 2001. What causes the unfrozen water in polymers: Hydrogen bonds between water and polymer chains? Polymer 42:3943-3947.
53. Ravivarapu HB, Burton K, DeLuca PP. 2000. Polymer and microsphere blending to alter the release of a peptide from PLGA microspheres. Eur J Pharm Biopharm 50:263-270.
54. Iyer SS, Barr WH, Karnes HT. 2006. Profiling in vitro drug release from subcutaneous implants: A review of current status and potential implications on drug product development. Biopharm Drug Dispos 27:157-170.