Online citations, reference lists, and bibliographies.
← Back to Search

Biocompatibility Of An Injectable In Situ Forming Depot For Peptide Delivery.

K. Schoenhammer, J. Boisclair, H. Schütz, H. Petersen, A. Goepferich
Published 2010 · Chemistry, Medicine

Cite This
Download PDF
Analyze on Scholarcy
Share
Poly(ethyleneglycol) 500 dimethylether (PEG500DME) was tested as a novel solvent for the manufacture of an injectable in situ forming depot (ISFD) containing poly(D,L-lactide-co-glycolide) (PLGA). The sustained release of pasireotide from the ISFD was evaluated in vitro and in vivo. Furthermore, the local tolerability of the delivery system using PEG500DME was investigated in subcutaneous (s.c.) tissue over 48 days. A flow-through cell was used to determine the in vitro drug release from the ISFD in comparison to a peptide suspension without polymer. The biocompatibility as well as the pharmacokinetic profile of the ISFD was investigated in rabbits. A prolonged peptide release over at least 48 days with an initial burst lower than 1% was observed in vitro for the ISFD compared to the suspension without polymer. A similar tissue response as it was observed for other common PLGA delivery systems was found upon histopathological examination of tissue from the administration site in rabbits. A sustained release of at least 48 days in vivo confirmed the in vitro observation including the low initial plasma concentration levels. Two ISFDs with different peptide loads were used to correlate the in vitro and in vivo data (IVIVC). Overall, the functionality of the ISFD containing PEG500DME as a novel solvent was demonstrated in vitro and in vivo. In addition, the local tolerability of the system confirmed the biocompatibility of PEG500DME in parenteral depots.
This paper references
10.1016/S0142-9612(00)00101-0
Synthetic biodegradable polymers as orthopedic devices.
J. C. Middleton (2000)
10.1016/S0142-9612(00)00040-5
Influence of particle size and dissolution conditions on the degradation properties of polylactide-co-glycolide particles.
M. Dunne (2000)
10.1016/J.IJPHARM.2007.10.016
Controlled release of growth hormone from thermosensitive triblock copolymer systems: In vitro and in vivo evaluation.
Sibao Chen (2008)
10.1016/j.ejpb.2009.08.007
Application of electron paramagnetic resonance (EPR) spectroscopy and imaging in drug delivery research - chances and challenges.
Sabine Kempe (2010)
10.1021/MA961627Y
Polymer Bulk Erosion
A. Göpferich (1997)
10.1016/S0378-5173(00)00568-8
Myotoxicity studies of injectable biodegradable in-situ forming drug delivery systems.
H. Kranz (2001)
10.1016/j.ejpb.2009.06.008
Non-invasive in vivo evaluation of in situ forming PLGA implants by benchtop magnetic resonance imaging (BT-MRI) and EPR spectroscopy.
Sabine Kempe (2010)
10.1002/(SICI)1097-4636(19990605)45:3<231::AID-JBM11>3.0.CO;2-H
Biocompatibility of a biodegradable in situ forming implant system in rhesus monkeys.
M. A. Royals (1999)
10.1007/s11095-009-9969-0
Poly(ethyleneglycol) 500 Dimethylether as Novel Solvent for Injectable In Situ Forming Depots
K. Schoenhammer (2009)
10.1016/S0749-8063(98)70099-4
Orthopaedic applications for PLA-PGA biodegradable polymers.
K. Athanasiou (1998)
10.1016/j.ijpharm.2008.12.019
Injectable in situ forming depot systems: PEG-DAE as novel solvent for improved PLGA storage stability.
K. Schoenhammer (2009)
10.1007/BF01062126
Pharmacokinetic evaluation of stable piecewise cubic polynomials as numerical integration functions
K. Yeh (2005)
10.1016/S0939-6411(97)00065-9
Pharmacological modulation of the tissue response to implanted polylactic-co-glycolic acid microspheres
A. Daugherty (1997)
10.1023/A:1020730102176
Assuring Quality and Performance of Sustained and Controlled Release Parenterals: AAPS Workshop Report, Co-Sponsored by FDA and USP
D. Burgess (2004)
10.1016/J.EJPS.2004.03.001
Assuring quality and performance of sustained and controlled released parenterals.
D. Burgess (2004)
10.1002/jps.21415
Changes in morphology of in situ forming PLGA implant prepared by different polymer molecular weight and its effect on release behavior.
Reyhaneh Astaneh (2009)
10.1016/j.jconrel.2008.04.004
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.
M. Martinez (2008)
10.1016/S0168-1656(00)00409-0
Versatility of biodegradable biopolymers: degradability and an in vivo application.
V. Hasirci (2001)
10.1016/j.addr.2012.09.004
Biodegradation and biocompatibility of PLA and PLGA microspheres.
Shive (1997)
10.1208/pt010101
Sustained activity and release of leuprolide acetate from an in situ forming polymeric implant
H. Ravivarapu (2008)
10.1016/j.jconrel.2008.01.004
Evaluation of in vivo-in vitro release of dexamethasone from PLGA microspheres.
B. S. Zolnik (2008)
10.1016/J.IJPHARM.2006.07.051
Phase-sensitive polymer-based controlled delivery systems of leuprolide acetate: in vitro release, biocompatibility, and in vivo absorption in rabbits.
S. Singh (2007)
10.1007/s11095-007-9478-y
In Vitro and In Vivo Drug Release from a Novel In Situ Forming Drug Delivery System
H. Kranz (2007)
10.1208/s12249-008-9126-9
Formulation and Evaluation of PLA and PLGA In Situ Implants Containing Secnidazole and/or Doxycycline for Treatment of Periodontitis
H. Gad (2008)



This paper is referenced by
10.1016/j.ejps.2010.09.008
PLGA:poloxamer blend micro- and nanoparticles as controlled release systems for synthetic proangiogenic factors.
Yolanda Parajó (2010)
10.1089/jir.2011.0034
Microencapsulation of alpha interferons in biodegradable microspheres.
V. Sáez (2012)
10.1002/dta.2400
Sensitive quantification of the somatostatin analog AP102 in plasma by ultra-high pressure liquid chromatography-tandem mass spectrometry and application to a pharmacokinetic study in rats.
Philippe J Eugster (2018)
10.1016/j.ijpharm.2018.07.013
In‐situ forming PLGA implants for intraocular dexamethasone delivery
C. Bode (2018)
10.1016/j.jconrel.2013.12.020
Solvent induced phase inversion-based in situ forming controlled release drug delivery implants.
R. Thakur (2014)
10.1016/j.drudis.2013.09.001
Phage display as a technology delivering on the promise of peptide drug discovery.
Maryam Hamzeh-Mivehroud (2013)
10.1002/jps.23634
Trehalose limits BSA aggregation in spray-dried formulations at high temperatures: implications in preparing polymer implants for long-term protein delivery.
K. Rajagopal (2013)
10.1007/s13346-018-0491-y
In situ forming phase-inversion implants for sustained ocular delivery of triamcinolone acetonide
Ravi Sheshala (2018)
10.1016/j.jconrel.2013.08.024
PLGA in situ implants formed by phase inversion: critical physicochemical parameters to modulate drug release.
M. Parent (2013)
10.1016/S1773-2247(13)50048-7
Use of in vitro release models in the design of sustained and localized drug delivery systems for subcutaneous and intra-articular administration
S. Larsen (2013)
10.33980/jbcc.2019.v05i01.003
An Overview of In Situ Gel Forming Implants: Current Approach Towards Alternative Drug Delivery System
Nirmala Musmade (2019)
10.1016/j.ijpharm.2014.04.044
Injectable long-term control-released in situ gels of hydrochloric thiothixene for the treatment of schizophrenia: preparation, in vitro and in vivo evaluation.
Che Xin (2014)
Biocompatible zwitterionic polymer chemistries and hydrogels for gene therapy, drug delivery, and regenerative medicine
A. Sinclair (2016)
10.1517/17425247.2015.961420
Long-term delivery of protein therapeutics
Ravi Vaishya (2015)
10.1186/2008-2231-21-57
In-vitro/In-vivo comparison of leuprolide acetate release from an in-situ forming plga system
R. Mashayekhi (2012)
10.1016/j.drudis.2013.01.013
Injectable implants for the sustained release of protein and peptide drugs.
P. Agarwal (2013)
10.1002/jps.24546
Investigation of Fragment Antibody Stability and Its Release Mechanism from Poly(Lactide-co-Glycolide)-Triacetin Depots for Sustained-Release Applications.
Debby P Chang (2015)
Semantic Scholar Logo Some data provided by SemanticScholar