Title:Spray-dried Solid Lipid Nanoparticles for Enhancing Berberine Bioavailability
via Oral Administration
Volume: 29
Issue: 38
Author(s): Van Hong Nguyen*, Khoa Nguyen Manh Le and Mai Chau Ngoc Nguyen
Affiliation:
- Department of Life Sciences, Vietnam Academy of Science and Technology, University of Science and Technology of Hanoi, 18-
Hoang Quoc Viet, Cau Giay, Hanoi, Vietnam
Keywords:
Solid lipid nanoparticles, berberine, bioavailability, spray drying technique, ultrasonication, traditional medicine.
Abstract:
Background: Berberine (BBR), an Eastern traditional medicine, has expressed novel therapeutic activities,
especially for chronic diseases like diabetes, hyperlipemia, hypertension, and Alzheimer's disease.
However, the low oral bioavailability of BBR has limited the applications of these treatments. Hence, BBRloaded
solid lipid nanoparticles (BBR-SLNs) were prepared to improve BBR absorption into systemic circulations
via this route.
Methods: BBR-loaded solid lipid nanoparticles (BBR-SLNs) were prepared by ultrasonication and then transformed
into solid form via spray drying technique. The size morphology of BBR-SLNs was evaluated by dynamic
light scattering (DLS) and scanning electron microscope (SEM). Crystallinity of BBR and interaction
of BBR with other excipients were checked by spectroscopic methods. Entrapment efficiency of BBR-SLNs
as well as BBR release in gastrointestinal conditions were also taken into account. Lastly, SLN's cytotoxicity
for loading BBR was determined with human embryonic kidney cells (HEK293).
Results: Stearic acid (SA), glyceryl monostearate (GMS), and poloxamer 407 (P407) were selected for BBRSLNs
fabrication. BBR-SLNs had homogenous particle sizes of less than 200 nm, high encapsulation efficiency
of nearly 90% and loading capacity of above 12%. BBR-SLN powder could be redispersed without significant
changes in physicochemical properties and was stable for 30 days. Spray-dried BBR-SLNs showed a better
sustained in vitro release profile than BBR-SLNs suspension and BBR during the initial period, followed
by complete dissolution of BBR over 24 hours. Notably, cell viability on HEK293 even increased up to 150%
compared to the control sample at 100 μg/mL BBR-unloaded SLNs.
Conclusion: Hence, SLNs may reveal a promising drug delivery system to broaden BBR treatment for oral administration.
