In recent years, natural ingredients have gained importance for therapeutic treatment due to their minimal toxicity. However, the delivery of these phytoconstituents poses a challenge to provide better efficacy. Current research reports the development of nanoemulgel (NEG) loaded with ginger oleoresin (GOR) and lipid guggul extract (LGE) for the management of rheumatoid arthritis (RA). The nanoemulsion (NE) was developed using the spontaneous emulsification technique by the pseudo-ternary method. The optimized nanoemulsion exhibited globule size of 16.08±2.55, PDI of 0.187±0.06 and Zeta Potential of-22.4±0.31. The cumulative release from in-vitro diffusion studies at pH 7.4 was about 99.72±3.47%, 57.98±2.11% and 86.42±5.13% of 6-gingerol, E-guggulsterone and Z-guggulsterone respectively at the end of 24 hours. The ex vivo studies on porcine ear skin showed sustained release with 92.8±3.21% for 6-gingerol, 55.61±0.91% for E-guggulsterone, and 84.2±4.22% for Z-guggulsterone released at the end of 24 hours. The cell culture studies on RAW 264.7 cells indicated a robust inhibition of LPS-induced IL-6 and TNF-α production indicating its efficacy in the management of RA. The Preclinical studies on male Wistar rats suggests that the developed NEG exhibited a comparable decrease in paw edema inflammation as compared to the marketed diclofenac sodium gel. These encouraging results demonstrates the potential of the developed nanoemulgel containing combination of GOR and LGE for the management of RA.
Ginger oleoresin (GOR) and Fenugreek oil was kindly gifted from Sunpure Extracts Pvt Ltd, Delhi, India. Lipid guggul extract (LGE) was received as a gift sample from Arjuna Naturals Pvt Ltd, Kerala, India. Castor oil and Capmul MCM was gifted from Jayant Agro-Organic Ltd, Mumbai, India and Abitec Corporation, USA respectively. Tween 80 and Kolliphor EL was given as a gift sample from Mohini Organics, Ltd, India and BASF, Mumbai, India respectively. Carbopol Ultrez 10 NF was provided as a gift sample from Lubrizol Advanced Materials India Pvt Ltd. Oleic acid, Transcutol P and Propylene glycol was purchased from Otto Chemie Pvt Ltd, Mumbai. India.
Formulation development
Screening of oils, surfactants, and co-surfactants
As GOR and LGE are liquids, selection of oil phase and surfactant phase were determined on the miscibility of these phytoconstituents in numerous oils, surfactants, and co-surfactants. Castor oil and Fenugreek oil were selected as functional excipients as they are known for anti-inflammatory activity [21, 22]. However, these oils were not sufficient to form a clear and stable nanoemulsion. Therefore, various oils such as isopropyl myristate (IPM), oleic acid (OA), ethyl oleate (EO), Captex 200P(C-200P) and Capmul MCM(C-MCM) were screened to find the optimum ratio of oil mixture. Apart from this, other surfactants, and co-surfactants such as Transcutol P (TP), PEG-400, Tween 20 (T20), Tween 80 (T80), Span 80(S80), Propylene glycol (PG), Kolliphor ELP (K-ELP) were examined for selection of an appropriate Smix ratio.
Download the full research as PDF (before peer review) here: Development and preclinical assessment of nanoemulgel loaded with phytoconstituents for the management of rheumatoid arthritis
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Anita Chando, Vivek Basudkar, Sankalp Gharat et al. Development and preclinical assessment of nanoemulgel loaded with phytoconstituents for the management of rheumatoid arthritis, 09 May 2023, PREPRINT (Version 1) available at Research Square
https://doi.org/10.21203/rs.3.rs-2859476/v1
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