Development and evaluation in vitro and in vivo of injectable hydrolipidic gels with sustained-release properties for the management of articular pathologies such as osteoarthritis.
[en] This study aimed to evaluate glycerol monooleate (GMO) as a carrier to develop viscoelastic and injectable sustained-release drug delivery systems. The potential pro- and antioxidant activity of the developed hydrolipidic gels were evaluated by measuring the production of ROS by polymorphonuclear leukocytes (PMNs). In addition, the biocompatibility and effectiveness of two selected gel candidates were evaluated in vivo by evaluating the benefit of a single intraarticular injection of these new treatments in a model of osteoarthritis in rabbits. The in vitro study demonstrated that the carrier F1 did not have a pro-oxidative effect and even protected PMNs against natural auto-activation, regardless of the incorporation of either clonidine chlorhydrate or betamethasone dipropionate. The in vivo study demonstrated that F1 and F1-BDP induced a loss of cartilage quality in comparison to the control and reference groups but that the lesions of cartilage observed were generally mild, with not much full-depth erosion. Moreover, no exacerbating inflammation was observed when considering the synovial membranes and the PGE2 and CRP levels. These results seemed to demonstrate that the sustained-release formulation based on GMO could be well-tolerated after intraarticular injection. Moreover, it could have the potential to prevent inflammatory conditions while sustaining drug activity locally over weeks.
Disciplines :
Rheumatology
Author, co-author :
Réeff, Jonathan; Université Libre de Bruxelles - ULB > Laboratory of Pharmaceutics and Biopharmaceutics
Oprenyeszk, Frédéric ; Université de Liège > Département des sciences de la motricité > Unité de recherche sur l'os et le cartilage (U.R.O.C.)
Franck, Thierry ; Université de Liège > Centre de l'oxygène : Recherche et développement (C.O.R.D.)
Goole, Jonathan; Université Libre de Bruxelles - ULB > Laboratory of Pharmaceutics and Biopharmaceutics
De Vriese, Carine; Université Libre de Bruxelles - ULB > Laboratory of Pharmaceutics and Biopharmaceutics
Serteyn, Didier ; Université de Liège > Dép. clinique des animaux de compagnie et des équidés (DCA) > Anesthésiologie gén. et pathologie chirurg. des grds animaux
Henrotin, Yves ; Université de Liège > Département des sciences de la motricité > Unité de recherche sur l'os et le cartilage (U.R.O.C.)
Amighi, Karim; Université Libre de Bruxelles - ULB > Laboratory of Pharmaceutics and Biopharmaceutics
Language :
English
Title :
Development and evaluation in vitro and in vivo of injectable hydrolipidic gels with sustained-release properties for the management of articular pathologies such as osteoarthritis.
S. Abramson Drug delivery in degenerative joint disease: where we are and where to go? Adv. Drug Deliv. Rev. 58 2006 125 127
Aigner, T., Van Der Kraan, P., Van Den Berg, W., 2007. Osteoarthritis and inflammation -Inflammatory changes in osteoarthritic synoviopathy., in: J., B. (Ed.), Osteoarthritis, Inflammation and Degradation: A Continuum, pp. 219-235.
Aly, M.N., 2008. Intra-articular drug delivery: a fast growing approach. Recent patents on drug delivery & formulation 2, 231-237.
N. Bellamy, J. Campbell, V. Robinson, T. Gee, R. Bourne, and G. Wells Intraarticular corticosteroid for treatment of osteoarthritis of the knee Cochrane Database Syst. Rev. 2006 CD005328
N. Bellamy, J. Campbell, V. Robinson, T. Gee, R. Bourne, and G. Wells Viscosupplementation for the treatment of osteoarthritis of the knee Cochrane Database Syst. Rev. 2006 CD005328
N. Butoescu, O. Jordan, and E. Doelker Intra-articular drug delivery systems for the treatment of rheumatic diseases: a review of the factors influencing their performance Eur. J. Pharm. Biopharm.: Off. J. Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V 73 2009 205 218
R.T. Cook Alcohol abuse, alcoholism, and damage to the immune system-a review. Alcoholism clinical and experimental research 22 1998 1927 1942
J. Dong, D. Jiang, Z. Wang, G. Wu, L. Miao, and L. Huang Intra-articular delivery of liposomal celecoxib-hyaluronate combination for the treatment of osteoarthritis in rabbit model Int. J. Pharm. 441 2013 285 290
K. Edsman, H.R. Larkner, L.I. Nord, A. Karlsson, A. Wiebensjo, A.U. Hoglund, A.H. Kenne, and J. Nasstrom Intra-articular duration of DurolaneTM after single injection intorabbit knee Cartilage 2 2011 384 388
FDA, 1997. Food and Drug Administration - Guidance for Industry, Extended Release Oral Dosage Forms: Development, Evaluation, and Application of In Vitro/In Vivo Correlations, in: Services, D.o.H.a.H. (Ed.), Center for Drug Evaluation and Research.
Franck, T., Kohnen, S., Grulke, S., Neven, P., Goutman, Y., Peters, F., Pirotte, B., Deby-Dupont, G., Serteyn, D., 2008. Inhibitory effect of curcuminoids and tetrahydrocurcuminoids on equine activated neutrophils and myeloperoxidase activity. Physiological research/Academia Scientiarum Bohemoslovaca 57, 577-587.
A. Ganem-Quintanar, D. Quintanar-Guerrero, and P. Buri Monoolein: a review of the pharmaceutical applications Drug Dev. Ind. Pharm. 26 2000 809 820
P. Ghosh, and P.A. Cheras Vascular mechanisms in osteoarthritis. Best practice & research Clin. Rheumatol. 15 2001 693 709
P. Ghosh, and D. Guidolin Potential mechanism of action of intra-articular hyaluronan therapy in osteoarthritis: are the effects molecular weight dependent? Semin. Arthritis Rheumatism 32 2002 10 37
W. Goodwin, D. McCabe, E. Sauter, E. Reese, M. Walter, J.A. Buckwalter, and J.A. Martin Rotenone prevents impact-induced chondrocyte death J. Orthopaedic Res.: Off. Publ. Orthopaedic Res. Soc. 28 2010 1057 1063
Y. Henrotin, B. Kurz, and T. Aigner Oxygen and reactive oxygen species in cartilage degradation: friends or foes? Osteoarthritis Cartilage/OARS, Osteoarthritis Res. Soc. 13 2005 643 654
T. Kawano, H. Miura, T. Mawatari, T. Moro-Oka, Y. Nakanishi, H. Higaki, and Y. Iwamoto Mechanical effects of the intraarticular administration of high molecular weight hyaluronic acid plus phospholipid on synovial joint lubrication and prevention of articular cartilage degeneration in experimental osteoarthritis Arthritis Rheumatism 48 2003 1923 1929
S.J. Klebanoff Myeloperoxidase: friend and foe J. Leukocyte Biol. 77 2005 598 625
T. Kouno, T. Egashira, F. Takayama, Y. Kudo, and Y. Yamanaka Effect of methylprednisolone on plasma lipid peroxidation induced by lipopolysaccharide Jpn. J. Pharmacol. 64 1994 163 169
S. Laverty, C.A. Girard, J.M. Williams, E.B. Hunziker, and K.P. Pritzker The OARSI histopathology initiative - recommendations for histological assessments of osteoarthritis in the rabbit. Osteoarthritis and cartilage/OARS Osteoarthritis Res. Soc. 3 suppl 18 2010 S53 65
I.T. Lee, and C.M. Yang Role of NADPH oxidase/ROS in pro-inflammatory mediators-induced airway and pulmonary diseases Biochem. Pharmacol. 84 2012 581 590
M. Lotz Cytokines in cartilage injury and repair Clin. Orthopaedics Related Res. 2001 S108 115
N. Maricar, M.J. Callaghan, D.T. Felson, and T.W. O'Neill Predictors of response to intra-articular steroid injections in knee osteoarthritis-a systematic review Rheumatology 52 2013 1022 1032
Martin, J.A., McCabe, D., Walter, M., Buckwalter, J.A., McKinley, T.O., 2009. N-acetylcysteine inhibits post-impact chondrocyte death in osteochondral explants. The Journal of bone and joint surgery. American volume 91, 1890-1897.
F. Oprenyeszk, M. Chausson, V. Maquet, J.E. Dubuc, and Y. Henrotin Protective effect of a new biomaterial against the development of experimental osteoarthritis lesions in rabbit: a pilot study evaluating the intra-articular injection of alginate-chitosan beads dispersed in an hydrogel. Osteoarthritis and cartilage/OARS Osteoarthritis Res. Soc. 21 2013 1099 1107
M. Ouedraogo, R. Semde, I.T. Some, R. Traore-Ouedraogo, I.P. Guissou, V. Henschel, J. Dubois, K. Amighi, and B. Evrard Monoolein-water liquid crystalline gels of gentamicin as bioresorbable implants for the local treatment of chronic osteomyelitis: in vitro characterization Drug Dev. Ind. Pharm. 34 2008 753 760
Y.S. Park, S.W. Lim, I.H. Lee, T.J. Lee, J.S. Kim, and J.S. Han Intra-articular injection of a nutritive mixture solution protects articular cartilage from osteoarthritic progression induced by anterior cruciate ligament transection in mature rabbits: a randomized controlled trial Arthritis Res. Therapy 9 2007 R8
J.F. Pycock, W.E. Allen, and T.H. Morris Rapid, single-step isolation of equine neutrophils on a discontinuous Percoll density gradient Res. Vet. Sci. 42 1987 411 412
P. Ramakrishnan, B.A. Hecht, D.R. Pedersen, M.R. Lavery, J. Maynard, J.A. Buckwalter, and J.A. Martin Oxidant conditioning protects cartilage from mechanically induced damage J. Orthopaedic Re.:s Off. Publ. Orthopaedic Res. Soc. 28 2010 914 920
J. Reeff, A. Gaignaux, J. Goole, C. De Vriese, and K. Amighi New sustained-release intraarticular gel formulations based on monolein for local treatment of arthritic diseases Drug Dev. Ind. Pharm. 39 2012 1731 1741
J. Reeff, A. Gaignaux, J. Goole, J. Siepmann, F. Siepmann, C. Jerome, J.M. Thomassin, C. De Vriese, and K. Amighi Characterization and optimization of GMO-based gels with long term release for intraarticular administration Int. J. Pharm. 451 2013 95 103
H.I. Roach, T. Aigner, S. Soder, J. Haag, and H. Welkerling Pathobiology of osteoarthritis: pathomechanisms and potential therapeutic targets Curr. Drug Targets 8 2007 271 282
J. Samuels, S. Krasnokutsky, and S.B. Abramson Osteoarthritis: a tale of three tissues Bull. NYU Hospital Joint Dis. 66 2008 244 250
L.J. Sandell, and T. Aigner Articular cartilage and changes in arthritis. An introduction: cell biology of osteoarthritis Arthritis Res. 3 2001 107 113
N.L.J. Schneider, G. Deby-Dupont, and D. Serteyn Le rôle des synoviocytes dans l'articulation diarthrodiale enflammée Annales de Médecine Vétérinaire 151 2007 24 43
J.C. Shah, Y. Sadhale, and D.M. Chilukuri Cubic phase gels as drug delivery systems Adv. Drug Deliv. Rev. 47 2001 229 250
V.P. Shah, Y. Tsong, P. Sathe, and J.P. Liu In vitro dissolution profile comparison-statistics and analysis of the similarity factor, f2 Pharm. Res. 15 1998 889 896
Strober, W., 2001. Trypan blue exclusion test of cell viability. Current protocols in immunology / edited by John E. Coligan. [et al.] Appendix 3, Appendix 3B.
Z. Varga, E. Kosaras, E. Komodi, M. Katko, I. Karpati, J. Balla, G. Paragh, M.C. Aisa, and F. Galli Effects of tocopherols and 2,2'-carboxyethyl hydroxychromans on phorbol-ester-stimulated neutrophils J. Nutr. Biochem. 19 2008 320 327
G. Vilar, J. Tulla-Puche, and F. Albericio Polymers and drug delivery systems Curr. Drug Deliv. 9 2012 367 394
D. Wu, and A.I. Cederbaum Alcohol oxidative stress, and free radical damage Alcohol Res. Health: J. Natl. Institute Alcohol Abuse Alcoholism 27 2003 277 284
M. Yoshioka, R.D. Coutts, D. Amiel, and S.A. Hacker Characterization of a model of osteoarthritis in the rabbit knee. Osteoarthritis and cartilage/OARS Osteoarthritis Res. Soc. 4 1996 87 98
W. Zhang, G. Nuki, R.W. Moskowitz, S. Abramson, R.D. Altman, N.K. Arden, S. Bierma-Zeinstra, K.D. Brandt, P. Croft, M. Doherty, M. Dougados, M. Hochberg, D.J. Hunter, K. Kwoh, L.S. Lohmander, and P. Tugwell OARSI recommendations for the management of hip and knee osteoarthritis: part III: changes in evidence following systematic cumulative update of research published through January 2009. Osteoarthritis and cartilage/OARS Osteoarthritis Res. Soc. 18 2010 476 499
