Development and exploration on flowability of solid self-nanoemulsifying drug delivery system of morin hydrate

Morin hydrate (MH) is a promising flavonoid with diverse biological activities; unfortunately, it finds limited clinical application due to its low water solubility. Herein, we developed a liquid self nano-emulsifying drug delivery system (l-SNEDDS) employing Labrafil M 1944 CS, Cremophor RH 40, and Transcutol HP. The l-SNEDDS has been solidified by physical adsorption using inert carriers, i.e., Neusilin US2 and Aerosil 200. The S-SNEDDS was thoroughly investigated for flow function (FF), effective angle of wall friction (EAWF), and effective angle of internal friction (EAIF) employing a powder flow tester (PFT). The solid-state characterizations of S-SNEDDS were performed using FTIR, DSC, PXRD, and SEM. Further, in vitro dissolution, in vivo pharmacokinetic, and shelf life estimation were performed on selected SOF-2 formulation.

Highlights

• Solid SNEDDS of MH was prepared by physical adsorption method.

• Flowability of solid SNEDDS was investigated by powder flow tester.

• Solid state characterization confers transformation of crystalline to amorphous.

• In vitro-In vivo studies revealed an improvement of dissolution & bioavailability.

• The estimated shelf life of solid SNEDDS of MH was found to be 27.57 months.

The SOF-2 reveals good emulsifying ability, particle size (52 ± 4.25 nm), and PDI (0.133 ± 0.06). The FF and Jenike’s classification suggests the “free-flowing” nature of S-SNEDDS prepared using Neusilin US2. Further, S-SNEDDS prepared using Neusilin US2 showed a low friction angle, i.e., EAWF and EAIF, than Aerosil 200, therefore, a better flowability. The solid-state characterization of SOF-2 demonstrated the transition of MH from crystalline to amorphous state and good compatibility between MH and Neusilin US2. Further, SOF-2 showed more dissolution than pure MH and subsequently 2.97-fold increments in its oral bioavailability. Moreover, the shelf life of SOF-2 was reported to be 27.57 months, suggesting its excellent physical and chemical stability. In brief, solidifying l-SNEDDS and investigating flow behaviors by PFT could find attention in the pharmaceutical and food industry for commercial purposes.

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Pankaj V. Dangre, Shital B. Shinde, Sanjay J. Surana, Pankaj G. Jain, Shailesh S. Chalikwar,
Development and exploration on flowability of solid self-nanoemulsifying drug delivery system of morin hydrate,
Advanced Powder Technology,
Volume 33, Issue 8, 2022, 103716, ISSN 0921-8831,
https://doi.org/10.1016/j.apt.2022.103716.