Table 3.
Novel drug molecules and delivery system in OA treatment.
| Drugs | Delivery system | Physical properties | In vitro findings | Rat model | In vivo performance | Refers |
|---|---|---|---|---|---|---|
| rhSDF-1α | Fibrin/hyaluronic acid hydrogel | None | Sustained-release up to 14 days; biocompatible; recruit chondrogenic progenitor cell; regeneration of cartilage tissue |
None | None | Yu et al. (2015) |
| IGF-1 | PAMAM dendrimers | Generation 6: 58 kDa | No histotoxicity |
ACLT + MMx surgery | Penetrate cartilage; Sustained-release 30.4 days; rescue cartilage degeneration; reduces osteophyte formation |
Geiger et al. (2018) |
| BMP2 | GO flakes | Most abundant size: 1,598.5 nm | Sustained-release up to 40 days; inhibit inflammation; promote differentiation |
ACLT surgery | Histological improvement; inhibit inflammation |
Zhong et al. (2017) |
| TGF-β3 | GO 3D nano-scaffold | Average size 10–40 μm; drug adsorb >99 % |
Sustained-release up to 28 days; no cytotoxicity; promote chondrogenic differentiation |
None | None | Zhou et al. (2019) |
| Glutathione | Chitosan-gelatin based hydrogel | Pore size: 1.667 μm | No cytotoxicity; sustained-release up to 48 h; rescue oxidative damage; down-regulate inflammation |
None | None | Cheng et al. (2017) |
| KGN | PEG-PAMAM | Average size: 33.3– 36.4 nm; drug loading: 5.50 ± 0.23 (wt. %); Zeta potentials: +5 mV |
Low cytotoxicity; promote chondrogenic differentiation and ECM production; |
Healthy and 4% papain injection | Sustained-release up to 21 days | Hu et al. (2017) |
| NPPs | Average size: 320 nm; drug loading: 31.5% (w/w) |
Sustained release 62% drug in 3 months; bio-safe |
DMM surgery | Histological improvement; cartilage protection; inhibit inflammation |
Maudens et al. (2018) | |
| 3D Tri-Copolymer Scaffolds | Mean pore size: 20 to 30 µm | Up-regulate Acan, Sox9, and Col2a1; Low cytotoxicity; improve chondrogenesis |
None | None | Chen et al. (2021) | |
| TPCA-1 | Nanosomes | Average size: 50–200 nm | Low cytotoxicity; inhibit NO, LDH, PGE2, EPAS-1, MMP-13, ACAN and COL2A1 |
None | None | Bhatti et al. (2019) |
| Adenosine | PLA-b-PEG NPs | Diameter size: 129–144 nm | None | ACLT surgery | Inhibit NF-kb activation; chondroprotective; histological improvement |
Liu et al. (2019) |
| HCQ | CMFn nanocages | Diameter:22 nm; loading ratio: 48%; embedding ratio: 5% |
MMP-13/pH-responsive release; low cytotoxicity; increase Col2a1 and decrease inflammatory factors |
None | None | Chen et al. (2019) |
Abbreviations: rhSDF-1α): Human stromal cell-derived factor 1α; PAMAM: Amine terminal polyamidoamine; GO: Graphene oxide; KGN: Kartogenin; NPPs; nanocrystal–polymer particles; TPCA-1: [5-(p-Fluorophenyl)-2-ureido] thiophene-3-carboxamide; LDH: lactic dehydrogenase; PGE2: Prostaglandin E2; HCQ: hydroxychloroquine; CMFn: ferritin nanocages; DMM: Destabilization medial meniscus.