Developments in human growth hormone preparations: Sustained-release, prolonged half-life, novel injection devices, and alternative delivery routes

International Journal of Nanomedicine

Volumn 9, Issue 1, 2014, Pages 3527-3538

  Cai, Yunpeng ^a,b   Xu, Mingxin ^b   Yuan, Minglu ^b   Liu, Zhenguo ^a   Yuan, Weien ^b  

^a XINHUA HOSPITAL AFFILIATED TO SHANGHAI JIAO TONG UNIVERSITY SCHOOL OF MEDICINE   (China)

^b SHANGHAI JIAO TONG UNIVERSITY   (China)

Author keywords

Hydrogel; Intranasal; Microneedle; Microsphere; Pulmonary; Transdermal

Indexed keywords

HUMAN GROWTH HORMONE; MICROSPHERE; ZINC; DELAYED RELEASE FORMULATION; HYDROGEL;

COMPLEX FORMATION; DRUG BIOAVAILABILITY; DRUG DELIVERY DEVICE; DRUG DELIVERY SYSTEM; DRUG EFFICACY; DRUG FORMULATION; DRUG HALF LIFE; DRUG SAFETY; HUMAN; HYDROGEL; INTRANASAL DRUG DELIVERY SYSTEM; MEDICATION COMPLIANCE; MEMBRANE MICROPARTICLE; NEEDLE; NONHUMAN; PULMONARY DRUG DELIVERY SYSTEM; REVIEW; SUSTAINED DRUG RELEASE; SYRINGE; ADMINISTRATION AND DOSAGE; CHEMICAL STRUCTURE; CHEMISTRY; DELAYED RELEASE FORMULATION; DEVICES; PROCEDURES;

DELAYED-ACTION PREPARATIONS; DRUG DELIVERY SYSTEMS; HUMAN GROWTH HORMONE; HUMANS; HYDROGELS; MODELS, MOLECULAR; ZINC;

EID: 84905263431     PISSN: 11769114     EISSN: 11782013     Source Type: Journal    
DOI: 10.2147/IJN.S63507     Document Type: Review

References (79)

1. Strobl JS, Thomas MJ. Human growth hormone. Pharmacol Rev. 1994; 46(1): 1-34.
2. Webster R, Xie R, Didier E, et al. PEGylation of somatropin (recombinant human growth hormone): impact on its clearance in humans. Xenobiotica. 2008; 38(10): 1340-1351.
3. Hermanussen M, Geiger-Benoit K, Sippell WG. Catch-up growth following transfer from three times weekly im to daily sc administration of hGH in GH deficient patients, monitored by knemometry. Acta Endocrinol (Copenh). 1985; 109(2): 163-168.
4. Kapoor RR, Burke SA, Sparrow SE, et al. Monitoring of concordance in growth hormone therapy. Arch Dis Child. 2008; 93(2): 147-148.
5. Ho KK; 2007 GH Deficiency Consensus Workshop Participants. Consensus guidelines for the diagnosis and treatment of adults with GH deficiency II: a statement of the GH Research Society in association with the European Society for Pediatric Endocrinology, Lawson Wilkins Society, European Society of Endocrinology, Japan Endocrine Society, and Endocrine Society of Australia. Eur J Endocrinol. 2007; 157(6): 695-700.
6. Laursen T, Gravholt CH, Heickendorff L, et al. Long-term effects of continuous subcutaneous infusion versus daily subcutaneous injections of growth hormone (GH) on the insulin-like growth factor system, insulin sensitivity, body composition, and bone and lipoprotein metabolism in GH-deficient adults. J Clin Endocrinol Metab. 2001; 86(3): 1222-1228.
7. Giavoli C, Cappiello V, Porretti S, et al. Growth hormone therapy in GH-deficient adults: continuous vs alternate-days treatment. Horm Metab Res. 2003; 35(9): 557-561.
8. Reiter EO, Attie KM, Moshang T, et al; Genentech, Inc.-Alkermes, Inc. Collaborative Study Group. A multicenter study of the efficacy and safety of sustained release GH in the treatment of naive pediatric patients with GH deficiency. J Clin Endocrinol Metab. 2001; 86(10): 4700-4706.
9. Cunningham BC, Mulkerrin MG, Wells JA. Dimerization of human growth hormone by zinc. Science. 1991; 253(5019): 545-548.
10. Cunningham BC, Bass S, Fuh G, Wells JA. Zinc mediation of the binding of human growth hormone to the human prolactin receptor. Science. 1990; 250(4988): 1709-1712.
11. Johnson OL, Cleland JL, Lee HJ, et al. A month-long effect from a single injection of microencapsulated human growth hormone. Nat Med. 1996; 2(7): 795-799.
12. Herbert P, Murphy K, Johnson O, et al. A large-scale process to produce microencapsulated proteins. Pharm Res. 1998; 15(2): 357-361.
13. Tracy MA. Development and scale-up of a microsphere protein delivery system. Biotechnol Prog. 1998; 14(1): 108-115.
14. Cawley P, Wilkinson I, Ross RJ. Developing long-acting growth hormone formulations. Clin Endocrinol (Oxf). 2013; 79(3): 305-309.
15. Kwak HH, Shim WS, Choi MK, et al. Development of a sustainedrelease recombinant human growth hormone formulation. J Control Release. 2009; 137(2): 160-165.
16. Johnson OL, Jaworowicz W, Cleland JL, et al. The stabilization and encapsulation of human growth hormone into biodegradable microspheres. Pharm Res. 1997; 14(6): 730-735.
17. Kim HK, Chung HJ, Park TG. Biodegradable polymeric microspheres with "open/closed" pores for sustained release of human growth hormone. J Control Release. 2006; 112(2): 167-174.
18. Vlugt-Wensink KD, de Vrueh R, Gresnigt MG, et al. Preclinical and clinical in vitro in vivo correlation of an hGH dextran microsphere formulation. Pharm Res. 2007; 24(12): 2239-2248.
19. Lee HJ, Riley G, Johnson O, et al. In vivo characterization of sustainedrelease formulations of human growth hormone. J Pharmacol Exp Ther. 1997; 281(3): 1431-1439.
20. Wei Y, Wang Y-X, Wang W, Ho SV, Wei W, Ma G-H. mPEG-PLA microspheres with narrow size distribution increase the controlled release effect of recombinant human growth hormone. J Mater Chem. 2011; 21(34): 12691-12699.
21. Kakizawa Y, Nishio R, Hirano T, et al. Controlled release of protein drugs from newly developed amphiphilic polymer-based microparticles composed of nanoparticles. J Control Release. 2010; 142(1): 8-13.
22. Kim SJ, Hahn SK, Kim MJ, Kim DH, Lee YP. Development of a novel sustained release formulation of recombinant human growth hormone using sodium hyaluronate microparticles. J Control Release. 2005; 104(2): 323-335.
23. Péter F, Bidlingmaier M, Savoy C, Ji HJ, Saenger PH. Three-year efficacy and safety of LB03002, a once-weekly sustained-release growth hormone (GH) preparation, in prepubertal children with GH deficiency (GHD). J Clin Endocrinol Metab. 2012; 97(2): 400-407.
24. Biller BM, Ji HJ, Ahn H, et al. Effects of once-weekly sustainedrelease growth hormone: a double-blind, placebo-controlled study in adult growth hormone deficiency. J Clin Endocrinol Metab. 2011; 96(6): 1718-1726.
25. Kelly CA, Howdle SM, Naylor A, et al. Stability of human growth hormone in supercritical carbon dioxide. J Pharm Sci. 2012; 101(1): 56-67.
26. Govardhan C, Khalaf N, Jung CW, et al. Novel long-acting crystal formulation of human growth hormone. Pharm Res. 2005; 22(9): 1461-1470.
27. Kim HK, Park TG. Microencapsulation of human growth hormone within biodegradable polyester microspheres: protein aggregation stability and incomplete release mechanism. Biotechnol Bioeng. 1999; 65(6): 659-667.
28. Yoo HS. Photo-cross-linkable and thermo-responsive hydrogels containing chitosan and Pluronic for sustained release of human growth hormone (hGH). J Biomater Sci Polym Ed. 2007; 18(11): 1429-1441.
29. Katakam M, Ravis WR, Golden DL, Banga AK. Controlled release of human growth hormone following subcutaneous administration in dogs. Int J Pharm. 1997; 152(1): 53-58.
30. Tae G, Kornfield JA, Hubbell JA. Sustained release of human growth hormone from in situ forming hydrogels using self-assembly of fluoroalkyl-ended poly(ethylene glycol). Biomaterials. 2005; 26(25): 5259-5266.
31. Shinde UP, Joo MK, Moon HJ, Jeong B. Sol-gel transition of PEG-PAF aqueous solution and its application for hGH sustained release. J Mater Chem. 2012; 22(13): 6072-6079.
32. Park MR, Chun C, Ahn SW, Ki MH, Cho CS, Song SC. Sustained delivery of human growth hormone using a polyelectrolyte complexloaded thermosensitive polyphosphazene hydrogel. J Control Release. 2010; 147(3): 359-367.
33. Park MR, Seo BB, Song SC. Dual ionic interaction system based on polyelectrolyte complex and ionic, injectable, and thermosensitive hydrogel for sustained release of human growth hormone. Biomaterials. 2013; 34(4): 1327-1336.
34. Lee J, Tan CY, Lee SK, Kim YH, Lee KY. Controlled delivery of heat shock protein using an injectable microsphere/hydrogel combination system for the treatment of myocardial infarction. J Control Release. 2009; 137(3): 196-202.
35. Brodbeck KJ, Pushpala S, McHugh AJ. Sustained release of human growth hormone from PLGA solution depots. Pharm Res. 1999; 16(12): 1825-1829.
36. García J, Dorta MJ, Munguía O, Llabrés M, Fariña JB. Biodegradable laminar implants for sustained release of recombinant human growth hormone. Biomaterials. 2002; 23(24): 4759-4764.
37. de Schepper J, Rasmussen MH, Gucev Z, Eliakim A, Battelino T. Longacting pegylated human GH in children with GH deficiency: a single-dose, dose-escalation trial investigating safety, tolerability, pharmacokinetics and pharmacodynamics. Eur J Endocrinol. 2011; 165(3): 401-409.
38. Clark R, Olson K, Fuh G, et al. Long-acting growth hormones produced by conjugation with polyethylene glycol. J Biol Chem. 1996; 271(36): 21969-21977.
39. Cox GN, Rosendahl MS, Chlipala EA, Smith DJ, Carlson SJ, Doherty DH. A long-acting, mono-PEGylated human growth hormone analog is a potent stimulator of weight gain and bone growth in hypophysectomized rats. Endocrinology. 2007; 148(4): 1590-1597.
40. Pasut G, Mero A, Caboi F, Scaramuzza S, Sollai L, Veronese FM. A new PEG-beta-alanine active derivative for releasable protein conjugation. Bioconjug Chem. 2008; 19(12): 2427-2431.
41. Magnusson JP, Bersani S, Salmaso S, Alexander C, Caliceti P. In situ growth of side-chain PEG polymers from functionalized human growth hormone-a new technique for preparation of enhanced protein-polymer conjugates. Bioconjug Chem. 2010; 21(4): 671-678.
42. Pai SS, Hammouda B, Hong K, Pozzo DC, Przybycien TM, Tilton RD. The conformation of the poly(ethylene glycol) chain in monoPEGylated lysozyme and mono-PEGylated human growth hormone. Bioconjug Chem. 2011; 22(11): 2317-2323.
43. Mero A, Schiavon M, Veronese FM, Pasut G. A new method to increase selectivity of transglutaminase mediated PEGylation of salmon calcitonin and human growth hormone. J Control Release. 2011; 154(1): 27-34.
44. Touraine P, D'Souza GA, Kourides I, et al; GH Lipoatrophy Study Group. Lipoatrophy in GH deficient patients treated with a long-acting pegylated GH. Eur J Endocrinol. 2009; 161(4): 533-540.
45. Poznansky MJ, Halford J, Taylor D. Growth hormone-albumin conjugates. Reduced renal toxicity and altered plasma clearance. FEBS Lett. 1988; 239(1): 18-22.
46. Osborn BL, Sekut L, Corcoran M, et al. Albutropin: a growth hormone-albumin fusion with improved pharmacokinetics and pharmacodynamics in rats and monkeys. Eur J Pharmacol. 2002; 456(1-3): 149-158.
47. Cleland JL, Geething NC, Moore JA, et al. A novel long-acting human growth hormone fusion protein (VRS-317): enhanced in vivo potency and half-life. J Pharm Sci. 2012; 101(8): 2744-2754.
48. Kim ES, Jang do S, Yang SY, et al. Controlled release of human growth hormone fused with a human hybrid Fc fragment through a nanoporous polymer membrane. Nanoscale. 2013; 5(10): 4262-4269.
49. Höybye C, Pfeiffer AFH, Ferone D, Gilfoyle D, Beckert M, Christiansen JS. OR03-5 A phase 2, multicenter, multiple-dose, open-label, parallelgroup, active controlled, safety, tolerability, pharmacokinetic and pharmacodynamic study of ACP-001 in adult patients with Growth Hormone Deficiency (AGHD). Growth Horm IGF Res. 2012; 22(Suppl 1): S8-S9.
50. Popovic V, Goth M, Vanuga P, et al. Once-weekly, CTP-modified hGH (MOD-4023) is effective in growth hormone deficient adults: a phase II, dose and frequency finding study. Presented at the 15th International and 14th European Congress of Endocrinology, Florence, Italy, May 5-9, 2012. Endocrine Abstracts. 2012; 29: OC10. 5.
51. Wilkinson IR, Ferrandis E, Artymiuk PJ, et al. A ligand-receptor fusion of growth hormone forms a dimer and is a potent long-acting agonist. Nat Med. 2007; 13(9): 1108-1113.
52. Baldwin PA, Klingbeil CK, Grimm CJ, Longenecker JP. The effect of sodium tauro-24, 25-dihydrofusidate on the nasal absorption of human growth hormone in three animal models. Pharm Res. 1990; 7(5): 547-552.
53. Hedin L, Olsson B, Diczfalusy M, et al. Intranasal administration of human growth hormone (hGH) in combination with a membrane permeation enhancer in patients with GH deficiency: a pharmacokinetic study. J Clin Endocrinol Metab. 1993; 76(4): 962-967.
54. Fisher AN, Farraj NF, O'Hagan DT, et al. Effect of l-α-lysophosphatidylcholine on the nasal absorption of human growth hormone in three animal species. Int J Pharm. 1991; 74(2-3): 147-156.
55. Daugherty AL, Liggitt HD, McCabe JG, Moore JA, Patton JS. Absorption of recombinant methionyl-human growth hormone (Met-hGH) from rat nasal mucosa. Int J Pharm. 1988; 45(3): 197-206.
56. Laursen T, Grandjean B, Jørgensen JO, Christiansen JS. Bioavailability and bioactivity of three different doses of nasal growth hormone (GH) administered to GH-deficient patients: comparison with intravenous and subcutaneous administration. Eur J Endocrinol. 1996; 135(3): 309-315.
57. Agerholm C, Bastholm L, Johansen PB, Nielsen MH, Elling F. Epithelial transport and bioavailability of intranasally administered human growth hormone formulated with the absorption enhancers didecanoylL-alpha-phosphatidylcholine and alpha-cyclodextrin in rabbits. J Pharm Sci. 1994; 83(12): 1706-1711.
58. Cheng YH, Dyer AM, Jabbal-Gill I, et al. Intranasal delivery of recombinant human growth hormone (somatropin) in sheep using chitosanbased powder formulations. Eur J Pharm Sci. 2005; 26(1): 9-15.
59. Aspden TJ, Illum L, Skaugrud O. Chitosan as a nasal delivery system: evaluation of insulin absorption enhancement and effect on nasal membrane integrity using rat models. Eur J Pharm Sci. 1996; 4(1): 23-31.
60. Steyn D, du Plessis L, Kotzé A. Nasal delivery of recombinant human growth hormone: in vivo evaluation with Pheroid technology and N-trimethyl chitosan chloride. J Pharm Pharm Sci. 2010; 13(2): 263-273.
61. Illum L, Farraj NF, Davis S, Johansen BR, O'Hagan DT. Investigation of the nasal absorption of biosynthetic human growth hormone in sheep-use of a bioadhesive microsphere delivery system. Int J Pharm. 1990; 63(3): 207-211.
62. Leitner VM, Guggi D, Krauland AH, Bernkop-Schnürch A. Nasal delivery of human growth hormone: in vitro and in vivo evaluation of a thiomer/glutathione microparticulate delivery system. J Control Release. 2004; 100(1): 87-95.
63. Levin G, Gershonowitz A, Sacks H, et al. Transdermal delivery of human growth hormone through RF-microchannels. Pharm Res. 2005; 22(4): 550-555.
64. Lee JW, Choi SO, Felner EI, Prausnitz MR. Dissolving microneedle patch for transdermal delivery of human growth hormone. Small. 2011; 7(4): 531-539.
65. Fukushima K, Ise A, Morita H, et al. Two-layered dissolving microneedles for percutaneous delivery of peptide/protein drugs in rats. Pharm Res. 2011; 28(1): 7-21.
66. Ito Y, Ohashi Y, Shiroyama K, Sugioka N, Takada K. Self-dissolving micropiles for the percutaneous absorption of recombinant human growth hormone in rats. Biol Pharm Bull. 2008; 31(8): 1631-1633.
67. Folkesson HG, Hedin L, Weström BR. Lung to blood passage of human growth hormone after intratracheal instillation: stimulation of growth in hypophysectomized rats. J Endocrinol. 1992; 134(2): 197-203.
68. Patton JS, McCabe JG, Hansen SE, Daugherty AL. Absorption of human growth hormone from the rat lung. Biotechnol Ther. 1988; 1(3): 213-228.
69. Colthorpe P, Farr SJ, Smith IJ, Wyatt D, Taylor G. The influence of regional deposition on the pharmacokinetics of pulmonary-delivered human growth hormone in rabbits. Pharm Res. 1995; 12(3): 356-359.
70. Bosquillon C, Préat V, Vanbever R. Pulmonary delivery of growth hormone using dry powders and visualization of its local fate in rats. J Control Release. 2004; 96(2): 233-244.
71. Walvoord EC, de la Peña A, Park S, et al. Inhaled growth hormone (GH) compared with subcutaneous GH in children with GH deficiency: pharmacokinetics, pharmacodynamics, and safety. J Clin Endocrinol Metab. 2009; 94(6): 2052-2059.
72. Jalalipour M, Najafabadi AR, Gilani K, Esmaily H, Tajerzadeh H. Effect of dimethyl-beta-cyclodextrin concentrations on the pulmonary delivery of recombinant human growth hormone dry powder in rats. J Pharm Sci. 2008; 97(12): 5176-5185.
73. Yuen KC, Amin R. Developments in administration of growth hormone treatment: focus on Norditropin ® Flexpro ®. Patient Prefer Adherence. 2011; 5: 117-124.
74. Fidotti E. A history of growth hormone injection devices. J Pediatr Endocrinol Metab. 2001; 14(5): 497-501.
75. Dahlgren J, Veimo D, Johansson L, Bech I. Patient acceptance of a novel electronic auto-injector device to administer recombinant human growth hormone: results from an open-label, user survey of everyday use. Curr Med Res Opin. 2007; 23(7): 1649-1655.
76. Cázares-Delgadillo J, Ganem-Rondero A, Kalia YN. Human growth hormone: new delivery systems, alternative routes of administration, and their pharmacological relevance. Eur J Pharm Biopharm. 2011; 78(2): 278-288.
77. Agersø H, Møller-Pedersen J, Cappi S, Thomann P, Jesussek B, Senderovitz T. Pharmacokinetics and pharmacodynamics of a new formulation of recombinant human growth hormone administered by ZomaJet 2 Vision, a new needle-free device, compared to subcutaneous administration using a conventional syringe. J Clin Pharmacol. 2002; 42(11): 1262-1268.
78. Kang J, Wu F, Cai Y, Xu M, Yuan W. Development of recombinant human growth hormone (rhGH) sustained-release microspheres by a novel low temperature aqueous phase/aqueous phase emulsion method. Eur J Pharm Sci. 2014; 62: 141-147.
79. Chantalat L, Jones ND, Korber F, Navaza J, Pavlovsky AG. The crystalstructure of wild-type growth-hormone at 2. 5 angstrom resolution. Protein Pept Lett. 1995; 2: 333-340.