Novel rhein integrate transphytosomes as non-invasive local therapy for osteoarthritis to ameliorate cartilage deterioration in MIA-arthritic rats.
Colloids Surf B Biointerfaces
; 202: 111713, 2021 Jun.
Article
en En
| MEDLINE
| ID: mdl-33780905
Rhein (RH), a natural chondroprotective agent, suffers from poor systemic availability (20-25%) after oral administration concomitant to side effects on the gastrointestinal tract and liver. We present a new approach for non-invasive local targeted delivery of rhein to ameliorate cartilage deterioration employing cartilage-homing phospholipids nanocarriers. This is the first work to elaborate RH loaded transphytosome (RH-T-PHY) as novel nanovesicular systems for transdermal drug delivery based on an advantageous hybrid between phytosomes and transfersomes or bilosomes. Here, we developed transphytosomes through incorporating various edge activators (EAs) such as Tween 80, Span 80 and sodium deoxycholate into the lipid bilayer of RH phytosomes to affix the flexibility. RH-T-PHY with high flexibility and entrapment efficacy showed the highest significant skin permeation compared to conventional phytosomes. Additionally, RH-T-PHY have a magnificent potential in maintaining high chondroprotective activity as demonstrated by enhanced repair, regeneration of chondrocytes and GAG formation in MIA-induced osteoarthritis (OA) rat model. Besides, histological examination of vital organs revealed the formulation safety. Confocal laser microscopy images revealed the highest drug availability in the articular cartilage of RH-T-PHY treated group. Conclusively, novel RH-T-PHY can serve as a promising alternative means for delivery of chondroprotective drugs for effective non-invasive local therapy of OA.
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Texto completo:
1
Bases de datos:
MEDLINE
Asunto principal:
Osteoartritis
/
Cartílago Articular
Límite:
Animals
Idioma:
En
Revista:
Colloids Surf B Biointerfaces
Asunto de la revista:
QUIMICA
Año:
2021
Tipo del documento:
Article