Poly(L-lactic acid) (PLA) |
Paclotaxel |
carrageenan induced rabbit model of arthritis/IA Injections |
20% paclitaxel loaded PLA microspheres in the 35-100 um size range delivered intra-articularly reduced all measure of inflammation |
[116] |
PLA |
Methotrexate (MTX) |
Rabbit induced arthritis model/IA Injections |
10 fold increase in MTX retention in joint compared to free MTX after intra articular injection |
[117] |
PLGA-PEG |
methacrylic derivative of ibuprofen |
Ex vivo sheep joints |
Decreased burst release of drug and prolonged sustained release for up to 3 months |
[118] |
PLGA |
Clonidine |
In vitro drug release |
Achieves controlled release for up to 30 days of hydrophilic drug |
[119] |
PLGA |
Lornoxicam |
Rat induced arthritis model/IA Injections |
Reduced drug plasma levels compared to free drug, retention time increased after intra-articular injections |
[120, 121] |
PLGA |
Naproxen Sodium |
Rabbit induced arthritis model via intra-articular injection of ovalbumin and Freud’s Complete Adjuvant/IA Injection |
Improved cure of articular arthritis when treated with PLGA loaded particles compared to BSA microspheres. |
[122] |
PLGA |
ibuprofen/Labrafil |
In vitro drug release |
Prolonged drug release with addition of labrafil |
[123] |
PLGA |
Methylpredniso lone (MP) |
Rat induced arthritis model/IA Injection |
Rapid increase in MP concentration in plasma at 30 minutes compared to MP suspension |
[124] |
PLGA |
Dexamethasone |
mouse dorsal air pouch model/local Injection |
Similar DXM release with varying polymer molecular weights |
[100] |
PLGA |
Betamethasone sodium phosphate (BSP) |
rat air-pouch model/antigen-induced arthritic rabbit model/local or IA Injection |
joint swelling significantly decreased at 21 days with administration of PLGA drug loaded particles |
[125] |
PLA and PLGA |
hyaluronate |
Arthritis and osteoarthritis rat models/IA Injection |
administration of particles did not worsen already altered articular tissues and did not cause inflammation in healthy rat knees |
[126] |
PLGA |
PTH(1-34) |
Papain-induced OA rat model/IA Injection |
Effect of PTH/PLGA microspheres on suppressing the OA progression was similar to that of a once-every-three-day injections |
[127] |
PLGA |
Sulforaphane (SFN) |
Surgically induced OA (ACL transection) in rats/local delivery (or injection) |
Treatment with SFN-PLGA microspheres inhibited the mRNA and protein expression of COX-2, ADAMTS-5 and MMP-2 induced by LPS in articular chondrocytes. Intra-articular SFN-PLGA microspheres delayed the progression of surgically induced OA in rat. |
[128] |
PLGA |
siRNA against TNF-a |
preclinical model of RA/local injection |
PLGA microspheres slowly released siRNAs effectively inhibited the expression of TNF-a in arthritic joints |
[129] |
Chitosan |
Flurbiprofin |
Rat knee joints/IA Injection |
significant extended release of flurbiprofen from microspheres in comparison with its solution |
[110] |