A Novel Solid Nanocrystals Self-Stabilized Pickering Emulsion Prepared by Spray-Drying with Hydroxypropyl-β-cyclodextrin as Carriers

Abstract

A drug nanocrystals self-stabilized Pickering emulsion (NSSPE) with a unique composition and microstructure has been proven to significantly increase the bioavailability of poorly soluble drugs. This study aimed to develop a new solid NSSPE of puerarin preserving the original microstructure of NSSPE by spray-drying. A series of water-soluble solid carriers were compared and then Box-Behnken design was used to optimize the parameters of spray-drying. The drug release and stability of the optimized solid NSSPE in vitro were also investigated. The results showed that hydroxypropyl-β-cyclodextrin (HP-β-CD), rather than solid carriers commonly used in solidification of traditional Pickering emulsions, was suitable for the solid NSSPE to retain the original appearance and size of emulsion droplets after reconstitution. The amount of HP-β-CD had more influences on the solid NSSPE than the feed rate and the inlet air temperature. Fluorescence microscopy, confocal laser scanning microscopy and scanning electron microscopy showed that the reconstituted emulsion of the solid NSSPE prepared with HP-β-CD had the same core-shell structure with a core of oil and a shell of puerarin nanocrystals as the liquid NSSPE. The particle size of puerarin nanocrystal sand interfacial adsorption rate also did not change significantly. The cumulative amount of released puerarin from the solid NSSPE had no significant difference compared with the liquid NSSPE, which were both significantly higher than that of puerarin crude material. The solid NSSPE was stable for 3 months under the accelerated condition of 75% relative humidity and 40 °C. Thus, it is possible todevelop the solid NSSPE preserving the unique microstructure and the superior properties in vitro of the liquid NSSPE for poorly soluble drugs.

Pueraria lobata Targeted Preparation Improves the Clinical Symptoms of Cervical Spondylosis by Regulating the Balance of Gut Microbiota

“…However, puerarin is water-insoluble, which is difficult to be absorbed after oral administration, with low absolute bioavailability. In recent years, there have been many studies on preparations to improve the bioavailability of puerarin, such as puerarin phospholipid complex [ 12 ] and puerarin solid self-microemulsion [ 13 ]. With the constant advances in nanoscience, biopharmaceuticals, and materials science, new drug carrier materials continue to emerge.…”

Progress of Drug Nanocrystal Self-Stabilized Pickering Emulsions: Construction, Characteristics In Vitro, and Fate In Vivo

“…Although spray drying and freeze drying have been frequently used to solidify Pickering emulsions [ 80 , 81 ], there are only a few studies on the drying of DNSPEs. Up to now, only spray-drying a puerarin DNSPE with HP-β-cyclodextrin as a carrier [ 82 ] and freeze-drying a curcumin DNSPE with mannitol as a lyoprotectant [ 37 ] have been reported. Considering that the stabilizers adsorbed at the interface of DNSPE droplets are different from macromolecules, further research is warranted to ascertain whether the carriers used for spray drying the lyoprotectants used for freeze drying for traditional Pickering emulsions are still suitable for DNSPEs.…”