Abstract
The discovery of a new pharmacological application of berberine hydrochloride (BH) made it more clinically valuable. However, the further development of BH was hampered by its short half-life and side effects after intravenous injection. To overcome these problems, a novel BH delivery system was developed using natural red blood cell membrane-camouflaged BH-loaded gelatin nanoparticles (RBGPs) to reduce the toxicity associated with injections and achieve sustained release. The size of the RBGPs was 260.3 ± 4.1 nm, with an obvious core–shell structure, and the membrane proteins of the RBGPs were mostly retained. The RBGP system showed significant immune-evading capabilities and little cytotoxicity to human embryonic kidney (HEK) 293T cells and LO2 cells. Finally, RBGPs improved the sustained releasing effect of BH significantly. When the cumulative release time reached 120 h, the cumulative release rate of RBGPs was 78.42%. In brief, RBGPs hold the potential to achieve long circulation and sustained-release of BH, avoid side effects caused by high plasma concentration in common injection formulations, and broaden the clinical applications of BH.
Highlights
Berberine hydrochloride (BH, C20H18ClNO4, molecular weight (MW) = 371.82) is a well-known active isoquinoline alkaloid widely used in traditional Chinese medicine (TCM)
In order to avoid the deficiency of the existing nano-dosage forms of BH, red blood cell membrane-camouflaged berberine hydrochloride-loaded gelatin nanoparticles (RBGPs) were prepared to achieve sustained releasing effects and reduce the toxicity associated with injections of BH in this paper (Figure 1)
The results showed red blood cell membrane-camouflaged BH-loaded gelatin nanoparticles (RBGPs) were stable for 7 days
Summary
The reported nano-dosage forms of BH still have low oral bioavailability and potential side effects after intravenous injections [9] They require long and frequent administration for the treatment of cardiovascular disease and cancer. Gelatin nanoparticles loaded with moxifloxacin were prepared using a modified two-step desolvation method This method could be used for effective ocular delivery and controlled release of drugs in the corneal eye layer [15]. In order to avoid the deficiency of the existing nano-dosage forms of BH, red blood cell membrane-camouflaged berberine hydrochloride-loaded gelatin nanoparticles (RBGPs) were prepared to achieve sustained releasing effects and reduce the toxicity associated with injections of BH in this paper (Figure 1). In order to remove the excess Cy5, the solution was washed with PBS by centrifuging (13,200 rpm, 10 min, 4 ◦C); this was repeated three times
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