In situ forming parenteral drug delivery systems: An overview

European Journal of Pharmaceutics and Biopharmaceutics

Volumn 58, Issue 2, 2004, Pages 445-455

  Packhaeuser, C B ^a   Schnieders, J ^a   Oster, C G ^a   Kissel, T ^a  

^a PHILIPPS UNIVERSITY MARBURG   (Germany)

Author keywords

Biodegradable polymers; In situ cross linking; In situ forming implants; Ion mediated gelation; Protein delivery systems; Solvent precipitation; Thermally induced gelation; Thermoplastic pastes

Indexed keywords

CYCLOSPORIN A; MACROGOL; MICROSPHERE; PACLITAXEL; POLYMER; TRIACETIN;

BIODEGRADABILITY; BIOMEDICAL ENGINEERING; CROSS LINKING; DRUG DELIVERY SYSTEM; DRUG FORMULATION; DRUG MANUFACTURE; DRUG RELEASE; DRUG STABILITY; GELATION; IMPLANT; LIPOPHILICITY; MACROMOLECULE; MOLECULE; PHARMACEUTICAL ENGINEERING; PHYSICAL CHEMISTRY; PLASTICITY; POLYMERIZATION; PRECIPITATION; REVIEW; SOLVENT EFFECT; THERMODYNAMICS; THERMOSTABILITY;

ANIMALS; BIODEGRADATION, ENVIRONMENTAL; DELAYED-ACTION PREPARATIONS; DRUG DELIVERY SYSTEMS; GELS; HUMANS; INJECTIONS; OINTMENTS; POLYMERS; PROTEINS;

EID: 3843091677     PISSN: 09396411     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.ejpb.2004.03.003     Document Type: Review

References (70)

1. Venter J.C., et al. The sequence of the human genome. Science. 291:(5507):2001;1304-1351
2. Heller J., Barr J., Ng S., Shen H.-R. Injectable semi-solid poly (ortho esters) for the controlled delivery of therapeutic agents: synthesis and applications. Drug Deliv. Technol. 2:(1):2002;38. See also pages 40-43
3. Tapanainen J., Hovatta O., Juntunen K., Martikainen H., Ratsula K., Tulppala M., Tuomivaara L. Subcutaneous goserelin versus intranasal buserelin for pituitary down-regulation in patients undergoing IVF: a randomized comparative study. Hum. Reprod. 8:(12):1993;2052-2055
4. Davies P.H., Stewart S.E., Lancranjan L., Sheppard M.C., Stewart P.M. Long-term therapy with long-acting octreotide (Sandostatin-LAR) for the management of acromegaly. Clin. Endocrinol. 48:(3):1998;311-316
5. Okada H., Heya T., Ogawa Y., Shimamoto T. One-month release injectable microcapsules of a luteinizing hormone-releasing hormone agonist (leuprolide acetate) for treating experimental endometriosis in rats. J. Pharmacol. Exp. Ther. 244:(2):1988;744-750
6. R.L. Dunn, A.J. Tipton, R.J. Harkrader, J.A. Rogers, Intragingival delivery systems containing chemotherapeutic agents for treatment of periodontal diseases, PCT Int. Appl., 9,200,718 (1992).
7. R.L. Dunn, J.P. English, D.R. Cowsar, D.P. Vanderbilt, Biodegradable in-situ forming implants and methods of producing the same, US Patent 4,938,763 (1990).
8. Sartor O. Eligard: leuprolide acetate in a novel sustained-release delivery system. Urology. 61:(2 Suppl 1):2003;25-31
9. G. Chen, P.R. Houston, L.W. Kleiner, J.C. Wright, Injectable depot compositions containing polymers and aromatic alcohols, PCT Int. Appl., 2,003,041,684 (2003).
10. J. Heller, S.Y. Ng, PEG-poly(ortho ester), PEG-poly(ortho ester)-PEG, and poly(ortho ester)-PEG-poly(ortho ester) block copolymers, US Patent 5,939,453 (1999).
11. R.C. Rathi, G.M. Zentner, B. Jeong, Biodegradable low molecular weight triblock lactide-glycolide-polyethylene glycol copolymers having reverse thermal gelation properties, US Patent 6,201,072 (2001).
12. R.S. Bezwada, Preparation of liquid copolymers of e-caprolactone and lactide, US Patent 5,442,033 (1995).
13. R.S. Bezwada, S.C. Arnold, S.W. Shalaby, B.L. Williams, Liquid absorbable copolymers for parenteral applications, Eur. Pat. Appl., 635,272 (1995).
14. Schwach-Abdellaoui K., Moreau M., Schneider M., Boisramc B., Gurny R. Controlled delivery of metoclopramide using an injectable semi-solid poly(ortho ester) for veterinary application. Int. J. Pharm. 248:(1-2):2002;31-37
15. Walter K.A., Cahan M.A., Gur A., Tyler B., Hilton J., Colvin O.M., Burger P.C., Domb A., Brem H. Interstitial taxol delivered from a biodegradable polymer implant against experimental malignant glioma. Cancer Res. 54:(8):1994;2207-2212
16. Winternitz C.I., Jackson J.K., Oktaba A.M., Burt H.M. Development of a polymeric surgical paste formulation for taxol. Pharm. Res. 13:(3):1996;368-375
17. Zhang X., Jackson J.K., Wong W., Min W., Cruz T., Hunter W.L., Burt H.M. Development of biodegradable polymeric paste formulations for taxol: an in vitro and in vivo study. Int. J. Pharm. 137:(2):1996;199-208
18. Dordunoo S.K., Oktaba A.M.C., Hunter W., Min W., Cruz T., Burt H.M. Release of taxol from poly(e-caprolactone) pastes: effect of water-soluble additives. J. Contr. Release. 44:(1):1997;87-94
19. Alonso P.E., Perula L.A., Rioja L.F. Pain-temperature relation in the application of local anaesthesia. Br. J. Plast. Surg. 46:(1):1993;76-78
20. Bernatchez S.F., Merkli A., Tabatabay C., Gurny R., Zhao Q.H., Anderson J.M., Heller J. Biotolerance of a semisolid hydrophobic biodegradable poly(ortho ester) for controlled drug delivery. J. Biomed. Mater. Res. 27:(5):1993;677-681
21. Ng S.Y., Vandamme T., Taylor M.S., Heller J. Synthesis and erosion studies of self-catalyzed poly(ortho ester)s. Macromolecules. 30:(4):1997;770-772
22. Merkli A., Heller J., Tabatabay C., Gurny R. Purity and stability assessment of a semi-solid poly(ortho ester) used in drug delivery systems. Biomaterials. 17:(9):1996;897-902
23. Heller J., Barr J., Ng S., Shen H.-R., Gurny R., Schwach-Abdelaoui K., Rothen-Weinhold A., Van De Weert M. Development of poly(ortho esters) and their application for bovine serum albumin and bupivacaine delivery. J. Control. Release. 78:(1-3):2002;133-141
24. Heller J., Barr J., Ng S.Y., Shen H.-R., Schwach-Abdellaoui K., Gurny R., Vivien-Castioni N., Loup P.J., Baehni P., Mombelli A. Development and applications of injectable poly(ortho esters) for pain control and periodontal treatment. Biomaterials. 23:(22):2002;4397-4404
25. Van De Weert M., Van Steenbergen M.J., Cleland J.L., Heller J., Hennink W.E., Crommelin D.J.A. Semisolid, self-catalyzed poly(ortho esters) as controlled-release systems: protein release and protein stability issues. J. Pharm. Sci. 91:(4):2002;1065-1074
26. Payne R.G., Mcgonigle J.S., Yaszemski M.J., Yasko A.W., Mikos A.G. Development of an injectable, in situ crosslinkable, degradable polymeric carrier for osteogenic cell populations. Part 2. Viability of encapsulated marrow stromal osteoblasts cultured on crosslinking poly(propylene fumarate). Biomaterials. 23:(22):2002;4373-4380
27. Hedberg E.L., Tang A., Crowther R.S., Carney D.H., Mikos A.G. Controlled release of an osteogenic peptide from injectable biodegradable polymeric composites. J. Control. Release. 84:(3):2002;137-150
28. Annavajjula D., Yim K., Rowe S.C., Rokovich J.A., Hubbell J.A. A Novel Drug Delivery System for Recombinant Human Growth Hormone with Photopolymerized Hydrogels. Proceedings - 28th International Symposium on Controlled Release of Bioactive Materials and Fourth Consumer and Diversified Products Conference. vol. 2:2001;. pp. 985-986
29. Sawhney A.S., Pathak C.P., Hubbell J.A. Bioerodible hydrogels based on photopolymerized poly(ethylene glycol)-co-poly(alpha-hydroxy acid) diacrylate macromers. Macromolecules. 26:(4):1993;581-587
30. Philbrook M., Lehnert S., Warnock D., Duan S., Enscore D., Roth L. Tissue-adherent depot for prevention of local tumor recurrence. Proceedings - 27th International Symposium on Controlled Release of Bioactive Materials. 2000;510-511
31. Qiu B., Stefanos S., Ma J., Lalloo A., Perry B.A., Leibowitz M.J., Sinko P.J., Stein S. A hydrogel prepared by in situ cross-linking of a thiol-containing poly(ethylene glycol)-based copolymer: a new biomaterial for protein drug delivery. Biomaterials. 24:(1):2002;11-18
32. Bernkop-Schnurch A., Hornof M., Zoidl T. Thiolated polymers-thiomers: synthesis and in vitro evaluation of chitosan-2-iminothiolane conjugates. Int. J. Pharm. 260:(2):2003;229-237
33. Krauland A.H., Leitner V.M., Bernkop-Schnuerch A. Improvement in the in situ gelling properties of deacetylated gellan gum by the immobilization of thiol groups. J. Pharm. Sci. 92:(6):2003;1234-1241
34. Qiu B., Stefanos S., Leibowitz M., Sinko P., Stein S. A Novel Injectable Polymer Hydrogel System - Depogel for Controlled Delivery of Small and Large Molecule Drugs. Proceedings - 28th International Symposium on Controlled Release of Bioactive Materials and Fourth Consumer & Diversified Products Conference. vol. 2:2001;. pp. 1009-1010
35. Leloup O., Renaud M.A., Chaput C., Chenite A., Desrosiers E.A., Shive M. Intramuscular Implantations of Thermogelling Chitosan-based Materials. Proceedings - 28th International Symposium on Controlled Release of Bioactive Materials and Fourth Consumer & Diversified Products Conference. vol. 1:2001;. pp. 261-262
36. Chenite A., et al. Novel injectable neutral solutions of chitosan form biodegradable gels in situ. Biomaterials. 21:(21):2000;2155-2161
37. Cohen S., Lobel E., Trevgoda A., Peled Y., novel A. in situ-forming ophthalmic drug delivery system from alginates undergoing gelation in the eye. J. Control. Release. 44:(2-3):1997;201-208
38. C.G. Oster, M. Wittmar, F. Unger, L. Barbu-Tudoran, A.K. Schaper T. Kissel, Design of Amine-modified graft polyesters for the effective gene delivery using DNA loaded nanoparticles. Pharm. Res. Prepublication date: 13 Feb 2004.
39. Quintanar-Guerrero D., Fessi H., Allemann E., Doelker E. Influence of stabilizing agents and preparative variables on the formation of poly(D,L-lactic acid) nanoparticles by an emulsification-diffusion technique. Int. J. Pharm. 143:(2):1996;133-141
40. Dunn R.L. The Atrigel Drug Delivery System. in: Drugs and the Pharmaceutical Sciences. vol. 126:2003;Dekker, New York, MA. pp. 647-655
41. Ravivarapu H.B., Moyer K.L., Dunn R.L. Parameters affecting the efficacy of a sustained release polymeric implant of leuprolide. Int. J. Pharm. 194:(2):2000;181-191
42. Ravivarapu H.B., Moyer K.L., Dunn R.L. Sustained activity and release of leuprolide acetate from an in situ forming polymeric implant. AAPS PharmSciTech. 1:(1):2000
43. Ravivarapu H.B., Moyer K.L., Dunn R.L. Sustained suppression of pituitary-gonadal axis with an injectable, in situ forming implant of leuprolide acetate. J. Pharm. Sci. 89:(6):2000;732-741
44. Chu F.M., Jayson M., Dineen M.K., Perez R., Harkaway R., Tyler R.C. A clinical study of 22.5 mg La-2550: a new subcutaneous depot delivery system for leuprolide acetate for the treatment of prostate cancer. J. Urol. 168:(3):2002;1199-1203
45. R.L. Dunn, J.S. Garrett, H. Ravivarapu, B.L. Chandrashekar, Polymeric delivery formulations of leuprolide with improved efficacy, US Patent 6,565,874 (2003).
46. Brodbeck K.J., Desnoyer J.R., Mchugh A.J. Phase inversion dynamics of PLGA solutions related to drug delivery. Part II. The role of solution thermodynamics and bath-side mass transfer. J. Control. Release. 62:(3):1999;333-344
47. Graham P.D., Brodbeck K.J., Mchugh A.J. Phase inversion dynamics of PLGA solutions related to drug delivery. J. Control. Release. 58:(2):1999;233-245
48. Kranz H., Brazeau G.A., Napaporn J., Martin R.L., Millard W., Bodmeier R. Myotoxicity studies of injectable biodegradable in-situ forming drug delivery systems. Int. J. Pharm. 212:(1):2001;11-18
49. Royals M.A., Fujita S.M., Yewey G.L., Rodriguez J., Schultheiss P.C., Dunn R.L. Biocompatibility of a biodegradable in situ forming implant system in rhesus monkeys. J. Biomed. Mater. Res. 45:(3):1999;231-239
50. Jain R.A., Rhodes C.T., Railkar A.M., Malick A.W., Shah N.H. Controlled delivery of drugs from a novel injectable in situ formed biodegradable PLGA microsphere system. J. Microencapsul. 17:(3):2000;343-362
51. Jain R.A., Rhodes C.T., Railkar A.M., Malick A.W., Shah N.H. Controlled release of drugs from injectable in situ formed biodegradable PLGA microspheres: effect of various formulation variables. Eur. J. Pharm. Biopharm. 50:(2):2000;257-262
52. Chen G., Priebe D., Bannister R., Baudouin K., Wright J., Kleiner L., Desjardin M., Lucas C. Sustained Release of a Small Molecule Drug, Bupivacaine, from ALZAMER Depot. Proceedings - 28th International Symposium on Controlled Release of Bioactive Materials and Fourth Consumer & Diversified Products Conference. vol. 2:2001;. pp. 962-963
53. Cleland J.L. Injectable Gels for Local and Systemic Delivery of Proteins. Proceedings - 28th International Symposium on Controlled Release of Bioactive Materials and Fourth Consumer & Diversified Products Conference. vol. 1:2001;. pp. 45-46
54. Duenas E., Okumu F., Daugherty A., Cleland J. Sustained Delivery of rhVEGF from a Novel Injectable Liquid, PLAD. Proceedings - 28th International Symposium on Controlled Release of Bioactive Materials and Fourth Consumer & Diversified Products Conference 2001. vol. 2:2001;. pp. 1041-1042
55. Okumu F.W., Daugherty A., Dao L., Fielder P.J., Brooks D., Sane S., Cleland J.L. Sustained Delivery of Growth Hormone from a Novel Injectable Liquid, PLA (poly(lactic acid)) Depot. Proceedings-28th International Symposium on Controlled Release of Bioactive Materials and Fourth Consumer & Diversified Products Conference. vol. 2:2001;. pp. 1029-1030
56. Okumu F.W., Dao Le N., Fielder P.J., Dybdal N., Brooks D., Sane S., Cleland J.L. Sustained delivery of human growth hormone from a novel gel system: SABER. Biomaterials. 23:(22):2002;4353-4358
57. Okumu F.W., Daugherty A., Dao L., Fielder P.J., Brooks D., Sane S., Sullivan S., Tipton A.J., Cleland J.L. Evaluation of the SABER Delivery System for Sustained Release of Growth Hormone - Formulation Design and In Vivo Assessment. Proceedings - 28th International Symposium on Controlled Release of Bioactive Materials and Fourth Consumer & Diversified Products Conference. vol. 2:2001;. pp. 1031-1032
58. M. Eligard™ 7,5 mg Package Insert (2002).
59. Wang L., Kleiner L., Venkatraman S. Structure formation in injectable poly(lactide-co-glycolide) depots. J. Control. Release. 90:(3):2003;345-354
60. Stile R.A., Burghardt W.R., Healy K.E. Synthesis and characterization of injectable poly(N-isopropylacrylamide)-based hydrogels that support tissue formation in vitro. Macromolecules. 32:(22):1999;7370-7379
61. Bochot A., Fattal E., Gulik A., Couarraze G., Couvreur P. Liposomes dispersed within a thermosensitive gel: a new dosage form for ocular delivery of oligonucleotides. Pharm. Res. 15:(9):1998;1364-1369
62. Yong C.S., Choi J.S., Quan Q.Z., Rhee J.D., Kim C.K., Lim S.J., Kim K.M., Oh P.S., Choi H.G. Effect of sodium chloride on the gelation temperature, gel strength and bioadhesive force of poloxamer gels containing diclofenac sodium. Int. J. Pharm. 226:(1-2):2001;195-205
63. Muller R.H., Ruhl D., Runge S., Schulze-Forster K., Mehnert W. Cytotoxicity of solid lipid nanoparticles as a function of the lipid matrix and the surfactant. Pharm. Res. 14:(4):1997;458-462
64. Wasan K.M., Subramanian R., Kwong M., Goldberg I.J., Wright T., Johnston T.P. Poloxamer 407-mediated alterations in the activities of enzymes regulating lipid metabolism in rats. J. Pharm. Pharm. Sci. 6:(2):2003;189-197
65. Jeong B., Bae Y.H., Lee D.S., Kim S.W. Biodegradable block copolymers as injectable drug-delivery systems. Nature. 388:(6645):1997;860-862
66. Jeong B., Choi Y.K., Bae Y.H., Zentner G., Kim S.W. New biodegradable polymers for injectable drug delivery systems. J. Control. Release. 62:(1-2):1999;109-114
67. Jeong B., Bae Y.H., Kim S.W. Thermoreversible gelation of PEG-PLGA-PEG triblock copolymer aqueous solutions. Macromolecules. 32:(21):1999;7064-7069
68. Y. Cha, Y.K. Choi, Y.H. Bae, Thermosensitive biodegradable polymers based on poly(ether-ester) block copolymers, PCT Int. Appl. 9,715,287 (1997).
69. Zentner G.M., et al. Biodegradable block copolymers for delivery of proteins and water-insoluble drugs. J. Control. Release. 72:(1-3):2001;203-215
70. Lee D.S. Functional Biodegradable Polymers for Drug Delivery. Proceedings - 8th Workshop on Advanced and Functional Polymer Materials. 2000;. pp. 109-137