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Title: Enhanced skin penetration of berberine from proniosome gel attenuates pain and inflammation in a mouse model of osteoarthritis.
Authors: Lee, Choon Keong 
Zhang, Shipin 
Venkatesan, Gopalakrishnan 
Chong, Suet Yen 
Wang, Jiong-Wei 
Goh, Wei Jiang 
Panczyk, Tomasz
Tay, Yi Zhen
Hu, Jun
Ng, Wai Kiong 
Wacker, Matthias G 
Toh, Wei Seong 
Pastorin, Giorgia 
Issue Date: 24-Feb-2022
Publisher: Royal Society of Chemistry (RSC)
Citation: Lee, Choon Keong, Zhang, Shipin, Venkatesan, Gopalakrishnan, Irsan, Chong, Suet Yen, Wang, Jiong-Wei, Goh, Wei Jiang, Panczyk, Tomasz, Tay, Yi Zhen, Hu, Jun, Ng, Wai Kiong, Wacker, Matthias G, Toh, Wei Seong, Pastorin, Giorgia (2022-02-24). Enhanced skin penetration of berberine from proniosome gel attenuates pain and inflammation in a mouse model of osteoarthritis.. Biomaterials Science. ScholarBank@NUS Repository.
Abstract: Dermal delivery of bioactive molecules remains an attractive route of administration in osteoarthritis (OA) due to the local accumulation of drugs while avoiding their systemic side effects. In this study we propose a proniosome gel comprising non-ionic surfactants that self-assemble into de-hydrated vesicles for the delivery of the natural anti-inflammatory compound berberine. By modulating the hydrating ability of the proniosome gel, berberine can be efficiently released with minimal mechanical force. A combination of sorbitan oleate (S80) and polyethlene glycol sorbitan monolaurate (T20) in a sorbitan stearate (S60)-based proniosome enables a readily hydrated gel to deliver berberine into the skin, as confirmed by ex vivo skin permeation studies. Concurrently, an in vitro model of OA using primary mouse chondrocytes demonstrated that the release of berberine at a concentration as low as 1 μg mL-1 is sufficient to restore the production of sulphated glycosaminoglycans (sGAG) to levels comparable to healthy chondrocytes while avoiding the cytotoxic concentrations (IC50 = 33 μg mL-1) on skin keratinocytes. In a mouse model of OA, the optimized formulation is able to attenuate inflammation and pain and minimize cartilage degeneration. Taken together, these data demonstrate the feasibility of adopting proniosome gels as a suitable platform to deliver active molecules for the management of osteoarthritis.
Source Title: Biomaterials Science
ISSN: 2047-4830
DOI: 10.1039/d1bm01733k
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