Comparative studies on glycerol monooleate- and phytantriol-based cubosomes containing oridonin in vitro and in vivo

To improve the solubility and bioavailability of oridonin (ORI), glycerol monooleate lipid (GMO)- or phytantriol (PYT)-Poloxamer 407-propylene glycol-water systems were firstly used to develop cubosomes containing ORI for oral delivery. These cubosomes prepared through the fragmentation of bulk gels under homogenization conditions of 1200 bar and nine cycles had a mean particle size of around 200 nm with narrow size distribution, and ORI encapsulation efficiency over 85%. Powder X-ray diffraction and differential scanning calorimetry indicated that ORI was in an amorphous or molecular form in the cubosomes. The internal structures of GMO- and PYT-based cubosomes were revealed by small-angle X-ray scattering as a bi-continuous cubic liquid crystalline phase with Im3m and Pn3m geometry, respectively. About 80% of ORI was released in vitro from GMO- and PYT-based cubosomes at 24 h, showing a sustained release kinetics fitted with Higuchi's equation. The pharmacokinetic study in rats showed that the PYT-based cubosomes significantly enhanced the adsorption of ORI as compared to the GMO-based cubosomes and ORI suspension, with evidence of longer half-life and greater relative bioavailability (p < 0.01). Therefore, the PYT-based cubosomes containing ORI might be proposed as a promising candidate carrier for the efficient delivery of drug with therapeutic treatment.

Medienart:

E-Artikel

Erscheinungsjahr:

2017

Erschienen:

2017

Enthalten in:

Zur Gesamtaufnahme - volume:22

Enthalten in:

Pharmaceutical development and technology - 22(2017), 3 vom: 16. Mai, Seite 322-329

Sprache:

Englisch

Beteiligte Personen:

Shi, Xuan [VerfasserIn]
Peng, Tingting [VerfasserIn]
Huang, Ying [VerfasserIn]
Mei, Liling [VerfasserIn]
Gu, Yukun [VerfasserIn]
Huang, Jiayuan [VerfasserIn]
Han, Ke [VerfasserIn]
Li, Ge [VerfasserIn]
Hu, Chunli [VerfasserIn]
Pan, Xin [VerfasserIn]
Wu, Chuanbin [VerfasserIn]

Links:

Volltext

Themen:

0APJ98UCLQ
3,7,11,15-tetramethyl-1,2,3-hexadecanetriol
8LVI07A72W
C4YAD5F5G6
Cubosomes
Diterpenes, Kaurane
Drug Carriers
Drugs, Chinese Herbal
Fatty Alcohols
Glycerides
Glycerol monooleate
Journal Article
Monoolein
Oridonin
Pharmacokinetics
Phytantriol
Sustained release

Anmerkungen:

Date Completed 20.03.2017

Date Revised 20.03.2017

published: Print-Electronic

Citation Status MEDLINE

doi:

10.3109/10837450.2015.1121496

funding:

Förderinstitution / Projekttitel:

PPN (Katalog-ID):

NLM255591659