Study on the stabilization mechanisms of wet-milled cepharanthine nanosuspensions using systematical characterization

Objectives: Stability issues are inevitable problems that are encountered in nanosuspension (NS) technology developments and in the industrial application of pharmaceuticals. This study aims to assess the stability of wet-milled cepharanthine NSs and elucidate the stabilization mechanisms of different stabilizers.Methods: The aggregation state was examined via scanning electron microscopy, laser diffraction, and rheometry. The zeta potential, stabilizer adsorption, surface tension, and drug-stabilizer interactions were employed to elucidate the stabilization mechanisms.Results: The results suggest that croscarmellose sodium (CCS), D-α-tocopherol polyethylene glycol 1000 succinate (TPGS), or polyvinyl pyrrolidone VA64 (PVP VA64) alone was able to prevent nanoparticle aggregation for at least 30 days. Attempts to evaluate the stability mechanisms of different stabilization systems revealed that CCS improved the steric-kinetic stabilization of the NSs, attributed to its high viscosity, swelling capacity, and physical barrier effects. In contrast, the excellent physical stability of TPGS systems was mainly due to the reduced surface tension and higher crystallinity. PVP VA64 can adsorb onto the surfaces of nanoparticles and stabilize the NS via steric forces.Conclusion: This study demonstrated the complex effects of CCS, TPGS, and PVP VA64 on cepharanthine NS stability and presented an approach for the rational design of stable NSs.

Medienart:

E-Artikel

Erscheinungsjahr:

2020

Erschienen:

2020

Enthalten in:

Zur Gesamtaufnahme - volume:46

Enthalten in:

Drug development and industrial pharmacy - 46(2020), 2 vom: 17. Feb., Seite 200-208

Sprache:

Englisch

Beteiligte Personen:

Fu, Tingting [VerfasserIn]
Gu, Xiangshuai [VerfasserIn]
Liu, Qiang [VerfasserIn]
Peng, Xiaodong [VerfasserIn]
Yang, Jianhong [VerfasserIn]

Links:

Volltext

Themen:

1406-18-4
3WJQ0SDW1A
7592YJ0J6T
Benzylisoquinolines
Carboxymethylcellulose Sodium
Cepharanthine
Excipients
FZ989GH94E
Journal Article
K679OBS311
Nanosuspensions
O03S90U1F2
Physical stability
Polyethylene Glycols
Polyethylene glycol 1000
Povidone
Stabilization mechanism
Suspensions
Tocophersolan
U076Q6Q621
Vitamin E
Wet milling

Anmerkungen:

Date Completed 16.11.2020

Date Revised 16.11.2020

published: Print-Electronic

Citation Status MEDLINE

doi:

10.1080/03639045.2020.1716370

funding:

Förderinstitution / Projekttitel:

PPN (Katalog-ID):

NLM305319825