1,875
Views
73
CrossRef citations to date
0
Altmetric
Reviews

Role of in vitro release models in formulation development and quality control of parenteral depots

, PhD DSc, , PhD, , PhD, , PhD & , PhD
Pages 1283-1295 | Published online: 26 Nov 2009

Bibliography

  • Larsen C, Østergaard J, Larsen SW, Intra-articular depot formulation principles: Role in the management of postoperative pain and arthritic disorders. J Pharm Sci 2008;97:4622-54
  • Berkland C, Pollauf E, Raman C, Macromolecule release from monodisperse PLG microspheres: Control of release rates and investigation of release mechanism. J Pharm Sci 2007;96:1176-91
  • Burgess DJ, Hussain AS, Ingallinera TS, Chen ML. Assuring quality and performance of sustained and controlled release parenterals: Workshop report. AAPS PharmSci 2002;4:E7
  • Burgess DJ, Crommelin DJ, Hussain AS, Chen ML. Assuring quality and performance of sustained and controlled released parenterals. Eur J Pharm Sci 2004;21:679-90
  • Martinez M, Rathbone M, Burgess D, Huynh M. In vitro and in vivo considerations associated with parenteral sustained release products: a review based upon information presented and points expressed at the 2007 Controlled Release Society Annual Meeting. J Control Release 2008;129:79-87
  • Siewert M, Dressman J, Brown CK, Shah VP. FIP/AAPS guidelines to dissolution/in vitro release testing of novel/special dosage forms. AAPS PharmSciTech 2003;4:E7
  • Uppoor VRS. Regulatory perspectives on in vitro (dissolution)/in vivo (bioavailability) correlations. J Control Release 2001;72:127-32
  • Woo BH, Kostanski JW, Gebrekidan S, Preparation, characterization and in vivo evaluation of 120-day poly(D,L-lactide) leuprolide microspheres. J Control Release 2001;75:307-15
  • Young D, Farrell C, Shepard T. In vitro/in vivo correlation for modified release injectable drug delivery systems. In: Burgess DJ, editor. Injectable dispersed systems. Formulation, processing, and performance. New York: Taylor & Francis Group, 2005. p. 159-76
  • Stevens LE, Missel PJ, Weiner AL. Controlled flow-through dissolution methodology: A high-performance system. Pharm Dev Technol 2008;13:135-53
  • Saarinen-Savolainen P, Jarvinen T, Taipale H, Urtti A. Method for evaluating drug release from liposomes in sink conditions. Int J Pharm 1997;159:27-33
  • Diaz RV, Llabres M, Evora C. One-month sustained release microspheres of I-125-bovine calcitonin - In vitro in vivo studies. J Control Release 1999;59:55-62
  • Washington C. Drug release from microdisperse systems - a critical-review. Int J Pharm 1990;58:1-12
  • D'Souza SS, Deluca PP. Methods to assess in vitro drug release from injectable polymeric particulate systems. Pharm Res 2006;23:460-74
  • Pedersen BT, Østergaard J, Larsen SW, Larsen C. Characterization of the rotating dialysis cell as an in vitro model potentially useful for simulation of the pharmacokinetic fate of intra-articularly administered drugs. Eur J Pharm Sci 2005;25:73-9
  • The dissolution procedure: development and validation. Pharmacopeial Forum 2005;31:1463
  • Tingstad JE, Riegelman S. Dissolution rate studies I. Design and evaluation of a continuous flow apparatus. J Pharm Sci 1970;59:692-6
  • Nicklasson M, Lindberg J, Borga B, A collaborative study of the in vitro dissolution of phenacetin crystals comparing the flow through method with the USP Paddle method. Int J Pharm 1991;69:255-64
  • Shah AC, Nelson KG. Evaluation of a convective diffusion drug dissolution rate model. J Pharm Sci 1975;64:1518-20
  • Nelson KG, Shah AC. Convective diffusion-model for a transport-controlled dissolution rate process. J Pharm Sci 1975;64:610-4
  • Stay MS, Xu J, Randolph TW, Barocas VH. Computer simulation of convective and diffusive transport of controlled-release drugs in the vitreous humor. Pharm Res 2003;20:96-102
  • Caldwell JR. Intra-articular corticosteroids - Guide to selection and indications for use. Drugs 1996;52:507-14
  • Davis JM, Matalon L, Watanabe MD, Blake L. Depot antipsychotic drugs - Place in therapy. Drugs 1994;47:741-73
  • Chien YM. Long-acting parenteral drug formulations. J Parenter Sci Technol 1981;35:106-39
  • Scholtz HE, Pretorius SG, Wessels DH, Becker RH. Pharmacokinetic and glucodynamic variability: assessment of insulin glargine, NPH insulin and insulin ultralente in healthy volunteers using a euglycaemic clamp technique 2. Diabetologia 2005;48:1988-95
  • Porter CJH, Charman SA. Lymphatic transport of proteins after subcutaneous administration. J Pharm Sci 2000;89:297-310
  • Levick JR. Microvascular architecture and exchange in synovial joints. Microcirculation 1995;2:217-33
  • Poli A, Scott D, Bertin K, Influence of actin cytoskeleton on intra-articular and interstitial fluid pressures in synovial joints. Microvasc Res 2001;62:293-305
  • Simkin PA, Nilson KL. Trans-synovial exchange of large and small molecules. Clin Rheum Dis 1981;7:99-129
  • Simkin PA, Benedict RS. Iodide and albumin kinetics in normal canine wrists and knees. Arthritis Rheum 1990;33:73-9
  • Weinberger A, Simkin PA. Plasma proteins in synovial fluids of normal human joints. Semin Arthritis Rheum 1989;19:66-76
  • Owen SG, Francis HW, Roberts MS. Disappearance kinetics of solutes from synovial fluid after intra-articular injection. Br J Clin Pharmacol 1994;38:349-55
  • Simkin PA, Wu MP, Foster DM. Articular pharmacokinetics of protein-bound antirheumatic agents. Clin Pharmacokinet 1993;25:342-50
  • Medlicott NJ, Waldron NA, Foster TP. Sustained release veterinary parenteral products. Adv Drug Deliv Rev 2004;56:1345-65
  • Aukland K, Reed RK. Interstitial-lymphatic mechanisms in the control of extracellular fluid volume. Physiol Rev 1993;73:1-78
  • Zuidema J, Kadir F, Titulaer HAC, Oussoren C. Release and absorption rates of intramuscularly and subcutaneously injected pharmaceuticals (II). Int J Pharm 1994;105:189-207
  • Ballard BE. Biopharmaceutical considerations in subcutaneous and intramuscular drug administration. J Pharm Sci 1968;57:357-78
  • Huang Y, Hubbard JW, Midha KK. The role of the lymphatic system in the presystemic absorption of fluphenazine after intramuscular administration of fluphenazine decanoate in rats. Eur J Pharm Sci 1995;3:15-20
  • Luo JP, Hubbard JW, Midha KK. The roles of depot injection sites and proximal lymph nodes in the presystemic absorption of fluphenazine decanoate and fluphenazine: ex vivo experiments in rats. Pharm Res 1998;15:1485-9
  • Fredholt K, Larsen DH, Larsen C. Modification of in vitro drug release rate from oily parenteral depots using a formulation approach. Eur J Pharm Sci 2000;11:231-7
  • Larsen DB, Fredholt K, Larsen C. Addition of hydrogen bond donating excipients to oil solution: effect on in vitro drug release rate and viscosity. Eur J Pharm Sci 2001;13:403-10
  • Larsen SW, Thomsen AE, Rinvar E, Effect of drug lipophilicity on in vitro release rate from oil vehicles using nicotinic acid esters as model prodrug derivatives. Int J Pharm 2001;216:83-93
  • Minto CF, Howe C, Wishart S, Pharmacokinetics and pharmacodynamics of nandrolone esters in oil vehicle: effects of ester, injection site and injection volume. J Pharmacol Exp Ther 1997;281:93-102
  • Tanaka T, Kobayash H, Okumura K, Biopharmaceutical studies on parenteral preparation - intramuscular absorption of drugs from oily solutions in rat. Chem Pharm Bull 1974;22:1275-84
  • Larsen SW, Østergaard J, Friberg-Johansen H, In vitro assessment of drug release rates from oil depot formulations intended for intra-articular administration. Eur J Pharm Sci 2006;29:348-54
  • Larsen SW, Frost AB, Østergaard J, On the mechanism of drug release from oil suspensions in vitro using local anesthetics as model drug compounds. Eur J Pharm Sci 2008;34:37-44
  • Larsen DB, Joergensen S, Olsen NV, In vivo release of bupivacaine from subcutaneously administered oily solution. Comparison with in vitro release. J Control Release 2002;81:145-54
  • Wissing SA, Kayser O, Muller RH. Solid lipid nanoparticles for parenteral drug delivery. Adv Drug Deliv Rev 2004;56:1257-72
  • Yaghmur A, Glatter O. Characterization and potential applications of nanostructured aqueous dispersions. Adv Colloid Interface Sci 2009;147-48:333-42
  • Metselaar JM, Storm G. Liposomes in the treatment of inflammatory disorders. Expert Opin Drug Deliv 2005;2:465-76
  • Torchilin VP. Recent advances with liposomes as pharmaceutical carriers. Nat Rev Drug Discov 2005;4:145-60
  • Dingle JT, Gordon JL, Hazleman BL, Novel treatment for joint inflammation. Nature 1978;271:372-3
  • Mantripragada S. A lipid based depot (DepoFoam® technology) for sustained release drug delivery. Prog Lipid Res 2002;41:392-406
  • Fong WK, Hanley T, Boyd BJ. Stimuli responsive liquid crystals provide `on-demand' drug delivery in vitro and in vivo. J Control Release 2009;135:218-26
  • Cavalli R, Caputo O, Gasco MR. Preparation and characterization of solid lipid nanospheres containing paclitaxel. Eur J Pharm Sci 2000;10:305-9
  • Heiati H, Tawashi R, Shivers RR, Phillips NC. Solid lipid nanoparticles as drug carriers 1. Incorporation and retention of the lipophilic prodrug 3′-azido-3′-deoxythymidine palmitate. Int J Pharm 1997;146:123-31
  • Heng D, Cutler DJ, Chan HK, What is a suitable dissolution method for drug nanoparticles? Pharm Res 2008;25:1696-701
  • Levy MY, Benita S. Drug release from submicronized o/w emulsion - a new in vitro kinetic evaluation model. Int J Pharm 1990;66:29-37
  • Bonacucina G, Cespi M, Misici-Falzi M, Palmieri GF. Colloidal Soft Matter as Drug Delivery System. J Pharm Sci 2009;98:1-42
  • Hitzman CJ, Wiedmann TS, Dai HQ, Elmquist WF. Measurement of drug release from microcarriers by microdialysis. J Pharm Sci 2005;94:1456-66
  • Anderson M, Omri A. The effect of different lipid components on the in vitro stability and release kinetics of liposome formulations. Drug Deliv 2004;11:33-9
  • Drummond DC, Noble CO, Hayes ME, Pharmacokinetics and in vivo drug release rates in liposomal nanocarrier development. J Pharm Sci 2008;97:4696-740
  • Jain JP, Modi S, Domb AJ, Kumar N. Role of polyanhydrides as localized drug carriers. J Control Release 2005;103:541-63
  • Heller J, Barr J, Ng SY, Poly(ortho esters): synthesis, characterization, properties and uses. Adv Drug Deliv Rev 2002;54:1015-39
  • Sinha VR, Bansal K, Kaushik R, Poly-epsilon-caprolactone microspheres and nanospheres: an overview. Int J Pharm 2004;278:1-23
  • Patil GV. Biopolymer albumin for diagnosis and in drug delivery. Drug Dev Res 2003;58:219-47
  • Kumar MNVR, Muzzarelli RAA, Muzzarelli C, Chitosan chemistry and pharmaceutical perspectives. Chem Rev 2004;104:6017-84
  • Shi Y, Li LC. Current advances in sustained-release systems for parenteral drug delivery. Expert Opin Drug Deliv 2005;2:1039-58
  • Freitas S, Merkle HP, Gander B. Microencapsulation by solvent extraction/evaporation: reviewing the state of the art of microsphere preparation process technology. J Control Release 2005;102:313-32
  • Jiang WL, Gupta RK, Deshpande MC, Schwendeman SP. Biodegradable poly(lactic-co-glycolic acid) microparticles for injectable delivery of vaccine antigens. Adv Drug Deliv Rev 2005;57:391-410
  • Berchane NS, Carson KH, Rice-Ficht AC, Andrews MJ. Effect of mean diameter and polydispersity of PLG microspheres on drug release: Experiment and theory. Int J Pharm 2007;337:118-26
  • Vert M, Schwach G, Engel R, Coudane J. Something new in the field of PLA/GA bioresorbable polymers? J Control Release 1998;53:85-92
  • Klose D, Siepmann F, Elkhamz K, Siepmann J. PLGA-based drug delivery systems: Importance of the type of drug and device geometry. Int J Pharm 2008;354:95-103
  • Faisant N, Siepmann J, Benoit JP. PLGA-based microparticles: elucidation of mechanisms and a new, simple mathematical model quantifying drug release. Eur J Pharm Sci 2002;15:355-66
  • Siepmann J, Faisant N, Akiki J, Effect of the size of biodegradable microparticles on drug release: experiment and theory. J Control Release 2004;96:123-34
  • Faisant N, Akiki J, Siepmann F, Effects of the type of release medium on drug release from PLGA-based microparticles: Experiment and theory. Int J Pharm 2006;314:189-97
  • Zolnik BS, Burgess DJ. Evaluation of in vivo-in vitro release of dexamethasone from PLGA microspheres. J Control Release 2008;127:137-45
  • Klose D, Azaroual N, Siepmann F, Towards more realistic in vitro release measurement techniques for biodegradable microparticles. Pharm Res 2009;26:691-9
  • Liu FI, Kuo JH, Sung KC, Hu OY. Biodegradable polymeric microspheres for nalbuphine prodrug controlled delivery: in vitro characterization and in vivo pharmacokinetic studies. Int J Pharm 2003;257:23-31
  • van Dijkhuizen-Radersma R, Wright SJ, Taylor LM, In vitro/in vivo correlation for C-14-methylated lysozyme release from poly(ether-ester) microspheres. Pharm Res 2004;21:484-91
  • Zhang PC, Chen LL, Gu WW, In vitro and in vivo evaluation of donepezil-sustained release microparticles for the treatment of Alzheimer's disease. Biomaterials 2007;28:1882-8
  • Nash RA. Suspensions. In: Swarbrick J, Boylan JC, editors. Encyclopedia of Pharmaceutical Technology. Second ed. Basel: Marcel Dekker, 2002. p. 2654-67
  • Akers MJ, Fites AL, Robinson RL. Formulation design and development of parenteral suspensions. J Parenter Sci Technol 1987;41:88-96
  • Packhaeuser CB, Schnieders J, Oster CG, Kissel T. In situ forming parenteral drug delivery systems: an overview. Eur J Pharm Biopharm 2004;58:445-55
  • Rothen-Weinhold A, Gurny R, Dahn M. Formulation and technology aspects of controlled drug delivery in animals. Pharm Sci Technol Today 2000;3:222-31
  • Yu LX, Foster TP, Sarver RW, Moseley WM. Preparation, characterization, and in vivo evaluation of an oil suspension of a bovine growth hormone releasing factor analog. J Pharm Sci 1996;85:396-401
  • Madan PL. Sustained-release drug delivery systems: Part V, parenteral products. Pharm Manuf 1985;2:51-7
  • Crommelin DJ. In vitro release studies on drugs suspended in non-polar media II. The release of paracetamol and chloramphenicol from suspensions in liquid paraffin. Int J Pharm 1980;6:29-42
  • Crommelin DJ. In vitro release studies on drugs suspended in non-polar media I. The release of sodium chloride from suspensions in liquid paraffin. Int J Pharm 1980;5:305-16
  • Stout PJ, Howard SA, Mauger JW. Dissolution of pharmaceutical suspensions. In: Swarbrick J, Boylan JC, editors. Encyclopedia of Pharmaceutical Technology. New York: Marcel Dekker, 1991. p. 169-92
  • Larsen SW, Østergaard E, Poulsen SV, Diflunisal salts of bupivacaine, lidocaine and morphine - Use of the common ion effect for prolonging the release of bupivacaine from mixed salt suspensions in an in vitro dialysis model. Eur J Pharm Sci 2007;31:172-9
  • Gietz U, Arvinte T, Mader E, Sustained release of injectable zinc-recombinant hirudin suspensions: development and validation of in vitro release model. Eur J Pharm Biopharm 1998;45:259-64
  • Sartor O. Eligard: Leuprolide acetate in a novel sustained-release delivery system. Urology 2003;61:25-31
  • Gehrke SH. Synthesis and properties of hydrogels used for drug delivery. In: Amidon GL, Lee PI, Topp EM, editors. Transport processes in pharmaceutical systems. New York: Marcel Dekker, Inc., 2000. p. 473-546
  • Van Tomme SR, Storm G, Hennink WE. In situ gelling hydrogels for pharmaceutical and biomedical applications. Int J Pharm 2008;355:1-18
  • Hatefi A, Amsden B. Biodegradable injectable in situ forming drug delivery systems. J Control Release 2002;80:9-28
  • Zentner GM, Rathi R, Shih c, Biodegradable block copolymers for delivery of proteins and water-insoluble drugs. J Control Release 2001;72:203-15
  • Chen S, Singh J. Controlled release of growth hormone from thermosensitive triblock copolymer systems: In vitro and in vivo evaluation. Int J Pharm 2008;352:58-65
  • McHugh AJ. The role of polymer membrane formation in sustained release drug delivery systems. J Control Release 2005;109:211-21
  • Brodbeck KJ, DesNoyer JR, McHugh AJ. 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 1999;62:333-44
  • Choi S, Baudys M, Kim SW. Control of blood glucose by novel GLP-1 delivery using biodegradable triblock copolymer of PLGA-PEG-PLGA in type 2 diabetic rats. Pharm Res 2004;21:827-31
  • Hyun H, Kim YH, Song IB, In vitro and in vivo release of albumin using a biodegradable MPEG-PCL diblock copolymer as an in situ gel-forming carrier. Biomacromolecules 2007;8:1093-100
  • Katakam M, Ravis WR, Banga AK. Controlled release of human growth hormone in rats following parenteral administration of poloxamer gels. J Control Release 1997;49:21-6
  • Haglund BO, Joshi R, Himmelstein KJ. An in situ gelling system for parenteral delivery. J Control Release 1996;41:229-35
  • Wang Y, Lapitsky Y, Kang CE, Shoichet MS. Accelerated release of a sparingly soluble drug from an injectible hyaluronan-methylcellulose hydrogel. J Control Release 2009;doi:10.1016/j.jconrel.2009.05.025
  • Singh S, Singh J. Phase-sensitive polymer-based controlled delivery systems of leuprolide acetate: In vitro release, biocompatibility, and in vivo absorption in rabbits. Int J Pharm 2007;328:42-8
  • Kempe S, Metz H, Mäder K. Do in situ forming PLG/NMP implants behave similar in vitro and in vivo? A non-invasive and quantitative EPR investigation on the mechanisms of the implant formation process J Control Release 2008;130:220-35
  • Graham PD, Brodbeck KJ, McHugh AJ. Phase inversion of PLGA solutions related to drug delivery. J Control Release 1999;58:233-45
  • Kranz H, Bodmeier R. A novel in situ forming drug delivery system for controlled parenteral drug delivery. Int J Pharm 2007;332:107-14
  • Plourde F, Motulsky A, Couffin-Hoarau A-L, First report on the efficacy of L-alanine-based in situ forming implants for the long-term parenteral delivery of drugs. J Control Release 2005;108:433-41
  • Vintiloiu A, Lafleur M, Bastiat G, Leroux J-C. In situ-forming oleogel implant for rivastigmine delivery. Pharm Res 2008;25:845-52
  • Okumu FW, Dao LN, Fielder PJ, Sustained delivery of human ghrowth hormone from a novel gel system: SABERTM. Biomaterials 2002;23:4353-8
  • Iyer SS, Barr WH, Karnes HT. Profiling in vitro drug release from subcutaneous implants: A review of current status and potential implications on drug product development. Biopharm Drug Dispos 2006;27:157-70
  • Iyer SS, Barr WH, Dance ME, A 'biorelevant' system to investigate in vitro drug released from a naltrexone implant. Int J Pharm 2007;340:104-18
  • James KC, Nicholls PJ, Roberts M. Biological half-lives of [4-14C]testosterone and some of its esters after injection into rat. J Pharm Pharmacol 1969;21:24-7
  • Hirano K, Ichihashi T, Yamada H. Studies on the absorption of practically water-insoluble drugs following injection V: subcutaneous absorption in rats from solutions in water immiscible oils. J Pharm Sci 1982;71:495-500
  • Larsen SW, Rinvar E, Svendsen O, Determination of the disappearance rate of iodine-125 labelled oils from the injection site after intramuscular and subcutaneous administration to pigs. Int J Pharm 2001;230:67-75
  • Schultz K, Mollgaard B, Fisher AN, Intramuscular rate of disappearance of oily vehicles in rabbits investigated by gamma-scintigraphy. Int J Pharm 1998;169:121-6
  • Anderson JM, Shive MS. Biodegradation and biocompatibility of PLA and PLGA microspheres. Adv Drug Deliv Rev 1997;28:5-24
  • Anderson JM. In-Vivo Biocompatibility of Implantable Delivery Systems and Biomaterials. Eur J Pharm Biopharm 1994;40:1-8
  • Swartz MA, Fleury ME. Interstitial flow and its effects in soft tissues. Annu Rev Biomed Eng 2007;9:229-56
  • Hwang CW, Wu D, Edelman ER. Impact of transport and drug properties on the local pharmacology of drug-eluting stents. Int J Cardiovasc Intervent 2003;5:7-12
  • D'Souza SS, Deluca PP. Development of a dialysis in vitro release method for biodegradable microspheres. AAPS PharmSciTech 2005;6
  • Kostanski JW, Deluca PP. A novel in vitro release technique for peptide containing biodegradable microspheres. AAPS PharmSciTech 2000;1:E4
  • Kim TK, Burgess DJ. Pharmacokinetic characterization C-14-vascular endothelial growth factor controlled release microspheres using a rat model. J Pharm Pharmacol 2002;54:897-905
  • Iyer SS, Barr WH, Karnes HT. A 'biorelevant' approach to accelerated in vitro drug release testing of a biodegradable, naltrexone implant. Int J Pharm 2007;340:119-25
  • Schliecker G, Schmidt C, Fuchs S, In vitro and in vivo correlation of buserelin release from biodegradable implants using statistical moment analysis. J Control Release 2004;94:25-37

Reprints and Corporate Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

To request a reprint or corporate permissions for this article, please click on the relevant link below:

Academic Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

Obtain permissions instantly via Rightslink by clicking on the button below:

If you are unable to obtain permissions via Rightslink, please complete and submit this Permissions form. For more information, please visit our Permissions help page.