Current advances in sustained-release systems for parenteral drug delivery

Major progresses in the development of parenteral sustained-release systems have been made in recent years as evidenced by the regulatory approval and market launch of several new products. Both the availability of novel carrier materials and the advances in method of fabrication have contributed to these commercial successes. With the formulation challenges associated with biologics, new delivery systems have also been evolved specifically to address the unmet needs in the parenteral sustained release of proteins. In this review paper, different new carriers systems and preparation methods are discussed with special focus on their applications to biologicals.

[1]  T. Kissel,et al.  Branched biodegradable polyesters for parenteral drug delivery systems. , 2000, Journal of controlled release : official journal of the Controlled Release Society.

[2]  J. Feijen,et al.  In vivo and in vitro degradation of poly(ether ester) block copolymers based on poly(ethylene glycol) and poly(butylene terephthalate). , 2004, Biomaterials.

[3]  Yi Yan Yang,et al.  Effect of polymer compositions on the fabrication of poly(ortho‐ester) microspheres for controlled release of protein , 2001 .

[4]  Sweta Modi,et al.  Role of polyanhydrides as localized drug carriers. , 2005, Journal of controlled release : official journal of the Controlled Release Society.

[5]  T. Hagen Liposomal cytokines in the treatment of infectious diseases and cancer. , 2005 .

[6]  J. Feijen,et al.  Microspheres for protein delivery prepared from amphiphilic multiblock copolymers. 2. Modulation of release rate. , 2000, Journal of controlled release : official journal of the Controlled Release Society.

[7]  H. Bunjes,et al.  Physicochemical characterization of lipid nanoparticles and evaluation of their drug loading capacity and sustained release potential , 1997 .

[8]  N. Elvassore,et al.  Production of Protein-Loaded Polymeric Microcapsules by Compressed CO2 in a Mixed Solvent , 2001 .

[9]  Sung Wan Kim,et al.  Controlled Release of Insulin from Injectable Biodegradable Triblock Copolymer Depot in ZDF Rats , 2003, Pharmaceutical Research.

[10]  N. Oku,et al.  Glucuronate-modified, long-circulating liposomes for the delivery of anticancer agents. , 2005, Methods in enzymology.

[11]  Martyn C. Davies,et al.  Supercritical fluid mixing: preparation of thermally sensitive polymer composites containing bioactive materials , 2001 .

[12]  J. Zhang,et al.  Development and characterization of a novel Cremophor EL free liposome-based paclitaxel (LEP-ETU) formulation. , 2005, European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V.

[13]  D. Crommelin,et al.  Liposomes as sustained release system for human interferon-gamma: biopharmaceutical aspects. , 2001, Biochimica et biophysica acta.

[14]  J. Cleland,et al.  Sustained delivery of human growth hormone from a novel gel system: SABER. , 2002, Biomaterials.

[15]  M. Radomsky,et al.  Sustained-Release Injectable Products , 2000 .

[16]  T. Kissel,et al.  In situ forming parenteral drug delivery systems: an overview. , 2004, European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V.

[17]  Lukchiu Li,et al.  Formulation and characterization of bupivacaine lipospheres. , 2004, International journal of pharmaceutics.

[18]  W. Hennink,et al.  IL-2 loaded dextran microspheres with attractive histocompatibility properties for local IL-2 cancer therapy. , 2003, Cytokine.

[19]  M Morlock,et al.  Erythropoietin loaded microspheres prepared from biodegradable LPLG-PEO-LPLG triblock copolymers: protein stabilization and in-vitro release properties. , 1998, Journal of controlled release : official journal of the Controlled Release Society.

[20]  Chun Xing Li Poly(L-glutamic acid)--anticancer drug conjugates. , 2002, Advanced drug delivery reviews.

[21]  Dennis Stephens,et al.  Polyanhydride implant for antibiotic delivery--from the bench to the clinic. , 2002, Advanced drug delivery reviews.

[22]  G. Gregoriadis,et al.  The effect of polysialylation on the immunogenicity and antigenicity of asparaginase: implication in its pharmacokinetics. , 2001, International journal of pharmaceutics.

[23]  J. Heller,et al.  Biochronomer™ technology , 2005, Expert opinion on drug delivery.

[24]  S. Lehnert,et al.  A novel non-toxic camptothecin formulation for cancer chemotherapy. , 2005, Biomaterials.

[25]  A. Gabizon Selective tumor localization and improved therapeutic index of anthracyclines encapsulated in long-circulating liposomes. , 1992, Cancer research.

[26]  D. Drucker,et al.  Development and characterization of a glucagon-like peptide 1-albumin conjugate: the ability to activate the glucagon-like peptide 1 receptor in vivo. , 2003, Diabetes.

[27]  Jan Feijen,et al.  Poly(ethylene oxide)/poly(butylene terephthalate) segmented block copolymers: the effect of copolymer composition on physical properties and degradation behavior , 2001 .

[28]  W. Hennink,et al.  Release of recombinant human interleukin-2 from dextran-based hydrogels. , 2002, Journal of controlled release : official journal of the Controlled Release Society.

[29]  R. Gurny,et al.  Release of BSA from poly(ortho ester) extruded thin strands. , 2001, Journal of controlled release : official journal of the Controlled Release Society.

[30]  K. Avgoustakis,et al.  Biodistribution properties of nanoparticles based on mixtures of PLGA with PLGA-PEG diblock copolymers. , 2005, International journal of pharmaceutics.

[31]  R B Greenwald,et al.  PEG drugs: an overview. , 2001, Journal of controlled release : official journal of the Controlled Release Society.

[32]  James C. Wright,et al.  Long-Term Controlled Delivery of Therapeutic Agents via an Implantable Osmotically Driven System: The DUROS Implant , 2002 .

[33]  J. Shah,et al.  Efficacy and Pharmacokinetics of Site-Specific Cefazolin Delivery Using Biodegradable Implants in the Prevention of Post-operative Wound Infections , 1998, Pharmaceutical Research.

[34]  Jingshe Song,et al.  Effect of Solid State Transition on the Physical Stability of Suspensions Containing Bupivacaine Lipid Microparticles , 2005, Pharmaceutical development and technology.

[35]  J. Benoit,et al.  Microencapsulation of protein particles within lipids using a novel supercritical fluid process. , 2002, International journal of pharmaceutics.

[36]  Y. Tsutsumi,et al.  Selective enhancement of thrombopoietic activity of PEGylated interleukin 6 by a simple procedure using a reversible amino‐protective reagent , 2001, British journal of haematology.

[37]  T. Kissel,et al.  Parenteral protein delivery systems using biodegradable polyesters of ABA block structure, containing hydrophobic poly(lactide-co-glycolide) A blocks and hydrophilic poly(ethylene oxide) B blocks , 1996 .

[38]  D. Collen,et al.  Clinical development of PEGylated recombinant staphylokinase (PEG-Sak) for bolus thrombolytic treatment of patients with acute myocardial infarction. , 2003, Advanced drug delivery reviews.

[39]  S. B. Tiwari,et al.  Potential Applications of Polymeric Microsphere Suspension as Subcutaneous Depot for Insulin , 2003, Drug development and industrial pharmacy.

[40]  Helmut Hahn,et al.  Atovaquone Nanosuspensions Show Excellent Therapeutic Effect in a New Murine Model of Reactivated Toxoplasmosis , 2001, Antimicrobial Agents and Chemotherapy.

[41]  G. Storm,et al.  Liposomes for Local Sustained Drug Release , 2000 .

[42]  Richard B Greenwald,et al.  Effective drug delivery by PEGylated drug conjugates. , 2003, Advanced drug delivery reviews.

[43]  L. Zarif,et al.  Elongated supramolecular assemblies in drug delivery. , 2002, Journal of controlled release : official journal of the Controlled Release Society.

[44]  M. Woodle,et al.  Controlling liposome blood clearance by surface-grafted polymers. , 1998, Advanced drug delivery reviews.

[45]  Hanry Yu,et al.  Polyphosphoester microspheres for sustained release of biologically active nerve growth factor. , 2002, Biomaterials.

[46]  H. Maeda,et al.  Mechanism of tumor-targeted delivery of macromolecular drugs, including the EPR effect in solid tumor and clinical overview of the prototype polymeric drug SMANCS. , 2001, Journal of controlled release : official journal of the Controlled Release Society.

[47]  Abraham J Domb,et al.  Polyanhydrides: an overview. , 2002, Advanced drug delivery reviews.

[48]  M. Bally,et al.  Preparation, characterization, and biological analysis of liposomal formulations of vincristine. , 2005, Methods in enzymology.

[49]  A. Cheung,et al.  Inhibition of neointimal hyperplasia in vascular grafts by sustained perivascular delivery of paclitaxel. , 2004, Kidney international.

[50]  Hua Yang,et al.  Biodegradable poly(epsilon-caprolactone)-poly(ethylene glycol) block copolymers: characterization and their use as drug carriers for a controlled delivery system. , 2003, Biomaterials.

[51]  G. Andriole,et al.  Safety and efficacy of an implantable leuprolide delivery system in patients with advanced prostate cancer. , 2000, The Journal of urology.

[52]  Y. Y. Yang,et al.  POE-PEG-POE triblock copolymeric microspheres containing protein. I. Preparation and characterization. , 2001, Journal of controlled release : official journal of the Controlled Release Society.

[53]  S. Kleppner,et al.  Implantable technology for long-term delivery of nalmefene for treatment of alcoholism. , 2004, International journal of pharmaceutics.

[54]  J. Benoit,et al.  Baclofen-loaded microspheres: preparation and efficacy testing in a new rabbit model. , 2005, European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V.

[55]  L. Webster,et al.  Relative analgesic potency of fentanyl and sufentanil during intermediate-term infusions in patients after long-term opioid treatment for chronic pain , 2004, Pain.

[56]  W. Hennink,et al.  Degradable dextran hydrogels: controlled release of a model protein from cylinders and microspheres. , 1999, Journal of controlled release : official journal of the Controlled Release Society.

[57]  N. Elvassore,et al.  Production of insulin-loaded poly(ethylene glycol)/poly(l-lactide) (PEG/PLA) nanoparticles by gas antisolvent techniques. , 2001, Journal of pharmaceutical sciences.

[58]  James M. Anderson,et al.  Biocompatibility of ABA triblock copolymer microparticles consisting of poly(l-lactic-co-glycolic-acid) A-blocks attached to central poly(oxyethylene) B-blocks in rats after intramuscular injection , 1997 .

[59]  S. Brosman,et al.  An open-label study of abarelix in men with symptomatic prostate cancer at risk of treatment with LHRH agonists. , 2003, Urology.

[60]  J. Mestecky,et al.  Biodegradable block copolymers for delivery of proteins and water-insoluble drugs. , 2001, Journal of controlled release : official journal of the Controlled Release Society.

[61]  K. Walter,et al.  Polilactofate microspheres for Paclitaxel delivery to central nervous system malignancies. , 2003, Clinical cancer research : an official journal of the American Association for Cancer Research.

[62]  O. Sartor Eligard: leuprolide acetate in a novel sustained-release delivery system. , 2003, Urology.

[63]  E Harper,et al.  Enhanced efficacy of a novel controlled release paclitaxel formulation (PACLIMER delivery system) for local-regional therapy of lung cancer tumor nodules in mice. , 1999, Clinical cancer research : an official journal of the American Association for Cancer Research.

[64]  O. Pérez,et al.  Proteoliposome derived cochleate as novel adjuvant. , 2006, Vaccine.

[65]  E. Schacht,et al.  Development of a poly(ortho ester) prototype with a latent acid in the polymer backbone for 5-fluorouracil delivery. , 2000, Journal of controlled release : official journal of the Controlled Release Society.

[66]  F. Veronese Peptide and protein PEGylation: a review of problems and solutions. , 2001, Biomaterials.

[67]  G. Gregoriadis,et al.  Polysialic acids: potential in drug delivery , 1993, FEBS letters.

[68]  L. Barbu-Tudoran,et al.  Design of Amine-Modified Graft Polyesters for Effective Gene Delivery Using DNA-Loaded Nanoparticles , 2004, Pharmaceutical Research.

[69]  Mathias Winterhalter,et al.  Stealth® liposomes: from theory to product , 1997 .

[70]  Kinam Park,et al.  A new microencapsulation method using an ultrasonic atomizer based on interfacial solvent exchange. , 2004, Journal of controlled release : official journal of the Controlled Release Society.

[71]  W. Hennink,et al.  In vitro biocompatibility of biodegradable dextran-based hydrogels tested with human fibroblasts. , 2001, Biomaterials.

[72]  B. Chertin,et al.  An implant releasing the gonadotropin hormone-releasing hormone agonist histrelin maintains medical castration for up to 30 months in metastatic prostate cancer. , 2000, The Journal of urology.

[73]  G. Gregoriadis,et al.  Improving the therapeutic efficacy of peptides and proteins: a role for polysialic acids. , 2005, International journal of pharmaceutics.

[74]  Robert Gurny,et al.  Poly(ortho esters): synthesis, characterization, properties and uses. , 2002, Advanced drug delivery reviews.

[75]  S. Mantripragada A lipid based depot (DepoFoam technology) for sustained release drug delivery. , 2002, Progress in lipid research.

[76]  Lukchiu Li,et al.  In Vitro Characterization of Polyorthoester Microparticles Containing Bupivacaine , 2003, Pharmaceutical development and technology.

[77]  Cleland,et al.  Recombinant human growth hormone poly(lactic-co-glycolic acid) microsphere formulation development. , 1997, Advanced drug delivery reviews.

[78]  D. Radulescu,et al.  Uniform Paclitaxel-Loaded Biodegradable Microspheres Manufactured by Ink-Jet Technology. , 2003 .

[79]  P. Caliceti,et al.  Pharmacokinetic and biodistribution properties of poly(ethylene glycol)-protein conjugates. , 2003, Advanced drug delivery reviews.

[80]  P. Caliceti,et al.  PEGylation of growth hormone-releasing hormone (GRF) analogues. , 2003, Advanced drug delivery reviews.

[81]  K. Jacobson,et al.  Cochleate lipid cylinders: formation by fusion of unilamellar lipid vesicles. , 1975, Biochimica et biophysica acta.

[82]  V. Sinha,et al.  Biodegradable microspheres for protein delivery. , 2003, Journal of controlled release : official journal of the Controlled Release Society.

[83]  G. Gregoriadis,et al.  Polysialylated insulin: synthesis, characterization and biological activity in vivo. , 2003, Biochimica et biophysica acta.

[84]  R. Duncan,et al.  Dextrins as potential carriers for drug targeting: tailored rates of dextrin degradation by introduction of pendant groups. , 2001, International journal of pharmaceutics.

[85]  Z. Gu,et al.  In vitro degradation and controlled release behavior of D,L-PLGA50 and PCL-b-D,L-PLGA50 copolymer microspheres. , 2005, Journal of controlled release : official journal of the Controlled Release Society.

[86]  J. Benoit,et al.  Development of novel 5-FU-loaded poly(methylidene malonate 2.1.2)-based microspheres for the treatment of brain cancers. , 2004, European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V.

[87]  J. M. Harris,et al.  Improvements in protein PEGylation: pegylated interferons for treatment of hepatitis C. , 2001, Journal of controlled release : official journal of the Controlled Release Society.

[88]  R. Kaushik,et al.  Poly-ϵ-caprolactone microspheres and nanospheres: an overview , 2004 .

[89]  J. Leroux,et al.  Novel injectable neutral solutions of chitosan form biodegradable gels in situ. , 2000, Biomaterials.

[90]  Y. Y. Yang,et al.  POE-PEG-POE triblock copolymeric microspheres containing protein. II. Polymer erosion and protein release mechanism. , 2001, Journal of controlled release : official journal of the Controlled Release Society.

[91]  V. Sinha,et al.  Biodegradable PEGylated microspheres and nanospheres , 2004 .

[92]  Constancis,et al.  Macromolecular Colloids of Diblock Poly(amino acids) That Bind Insulin. , 1999, Journal of colloid and interface science.

[93]  K. Leong,et al.  A novel biodegradable gene carrier based on polyphosphoester. , 2001, Journal of the American Chemical Society.

[94]  A. Domb,et al.  Preparation and Characterization of Carmustine Loaded Polyanhydride Wafers for Treating Brain Tumors , 1999, Pharmaceutical Research.

[95]  Chong-K. Kim,et al.  Effect of sodium chloride on the gelation temperature, gel strength and bioadhesive force of poloxamer gels containing diclofenac sodium. , 2001, International journal of pharmaceutics.

[96]  Y. Tsutsumi,et al.  Enhanced antitumor potency of polyethylene glycolylated tumor necrosis factor-alpha: a novel polymer-conjugation technique with a reversible amino-protective reagent. , 1999, The Journal of pharmacology and experimental therapeutics.

[97]  W. Hennink,et al.  Equilibrium water content of microspheres based on cross-linked dextran. , 1999, International journal of pharmaceutics.

[98]  W. E. Hennink,et al.  Effect of polymerization conditions on the network properties of dex-HEMA microspheres and macro-hydrogels. , 2005, International journal of pharmaceutics.

[99]  Willis,et al.  Ligand-targeted liposomes. , 1998, Advanced drug delivery reviews.

[100]  Horacio B Croxatto Progestin implants , 2000, Steroids.

[101]  T. Allen Ligand-targeted therapeutics in anticancer therapy , 2002, Nature Reviews Cancer.

[102]  T. Kissel,et al.  Biodegradable brush-like graft polymers from poly(d,l-lactide) or poly(d,l-lactide-co-glycolide) and charge-modified, hydrophilic dextrans as backbone—Synthesis, characterization and in vitro degradation properties , 1997 .

[103]  A. Göpferich,et al.  Lipid microparticles as a parenteral controlled release device for peptides. , 2001, Journal of controlled release : official journal of the Controlled Release Society.

[104]  Duu-Jong Lee,et al.  Gentamicin-loaded discs and microspheres and their modifications: characterization and in vitro release. , 2005, Journal of controlled release : official journal of the Controlled Release Society.

[105]  Mingshi Yang,et al.  Preparation and characterization of melittin-loaded poly (DL-lactic acid) or poly (DL-lactic-co-glycolic acid) microspheres made by the double emulsion method. , 2005, Journal of controlled release : official journal of the Controlled Release Society.

[106]  L. Zarif,et al.  Pharmacokinetics and tissue distribution after intravenous administration of a single dose of amphotericin B cochleates, a new lipid-based delivery system. , 2002, Journal of pharmaceutical sciences.

[107]  Imran Ahmad,et al.  Development and characterization of a novel liposome-based formulation of SN-38. , 2004, International journal of pharmaceutics.

[108]  L. Zarif Drug delivery by lipid cochleates. , 2005, Methods in enzymology.

[109]  C. Stevenson,et al.  An in vivo/in vitro comparison with a leuprolide osmotic implant for the treatment of prostate cancer. , 2001, Journal of controlled release : official journal of the Controlled Release Society.

[110]  W. Hennink,et al.  The use of aqueous PEG/dextran phase separation for the preparation of dextran microspheres. , 1999, International journal of pharmaceutics.

[111]  A. Gupte,et al.  Formulation and characterization of Paclitaxel, 5-FU and Paclitaxel + 5-FU microspheres. , 2004, International journal of pharmaceutics.

[112]  P. Sinko,et al.  A hydrogel prepared by in situ cross-linking of a thiol-containing poly(ethylene glycol)-based copolymer: a new biomaterial for protein drug delivery. , 2003, Biomaterials.

[113]  R. Mannino,et al.  Cochleate Delivery Vehicles: Applications in Vaccine Delivery , 2000 .

[114]  A. Göpferich,et al.  Development and characterization of lipid microparticles as a drug carrier for somatostatin. , 2001, International journal of pharmaceutics.

[115]  J. Shah,et al.  Local Delivery of Vancomycin for the Prophylaxis of Prosthetic Device-Related Infections , 2005, Pharmaceutical Research.

[116]  F. Dosio,et al.  Preparation, characterization, cytotoxicity and pharmacokinetics of liposomes containing docetaxel. , 2003, Journal of controlled release : official journal of the Controlled Release Society.

[117]  D. Attwood,et al.  The Release of 5-Fluorouracil from Microspheres of Poly(ε-Caprolactone-co-ethylene Oxide) , 2000 .

[118]  W. Saltzman,et al.  Pharmacokinetics of the Carmustine Implant , 2002, Clinical pharmacokinetics.

[119]  K. Shakesheff,et al.  The production of protein-loaded microparticles by supercritical fluid enhanced mixing and spraying. , 2005, Journal of controlled release : official journal of the Controlled Release Society.

[120]  J. Viret,et al.  Liposomes and virosomes as delivery systems for antigens, nucleic acids and drugs. , 2004, Current opinion in biotechnology.

[121]  B. Müller,et al.  Characterization of co-polymers of lactic and glycolic acid for supercritical fluid processing. , 2000, Biomaterials.

[122]  Q. Ye,et al.  DepoFoam technology: a vehicle for controlled delivery of protein and peptide drugs. , 2000, Journal of controlled release : official journal of the Controlled Release Society.

[123]  B. Gander,et al.  Importance of single or blended polymer types for controlled in vitro release and plasma levels of a somatostatin analogue entrapped in PLA/PLGA microspheres. , 2004, Journal of controlled release : official journal of the Controlled Release Society.

[124]  D. Grijpma,et al.  In vitro degradation of Polyactive 1000PEOT70PBT30 devices. , 2002, Biomaterials.

[125]  Robert Langer,et al.  Poly(anhydrides). 3. Poly(anhydrides) based on aliphatic-aromatic diacids , 1989 .

[126]  I. Goldberg,et al.  Poloxamer 407-mediated alterations in the activities of enzymes regulating lipid metabolism in rats. , 2003, Journal of pharmacy & pharmaceutical sciences : a publication of the Canadian Society for Pharmaceutical Sciences, Societe canadienne des sciences pharmaceutiques.

[127]  S. D'urso,et al.  Lipid microparticles as sustained release system for a GnRH antagonist (Antide). , 2003, Journal of controlled release : official journal of the Controlled Release Society.

[128]  Wenlei Jiang,et al.  Biodegradable poly(lactic-co-glycolic acid) microparticles for injectable delivery of vaccine antigens. , 2005, Advanced drug delivery reviews.

[129]  M. Whitlow,et al.  Prolonged circulating lives of single-chain Fv proteins conjugated with polyethylene glycol: a comparison of conjugation chemistries and compounds. , 1999, Bioconjugate chemistry.

[130]  J. Jansen,et al.  Histological evaluation of a biodegradable Polyactive/hydroxyapatite membrane. , 1995, Biomaterials.

[131]  I. Rubinstein,et al.  Liposomal vasoactive intestinal peptide. , 2005, Methods in enzymology.