Intranasal Delivery of Microspheres Loaded with 20 (R)-ginsenoside Rg3 Enhances Anti-Fatigue Effect in Mice.
Nasal delivery of 20 (R) -ginsenoside Rg3 (Rg3) has a short-lived anti-fatigue effect owing to rapid clearance by nasal cilia. Thus, in order to extend the residence time of Rg3 in the nasal cavity, a new drug delivery system is needed.



Chitosan microspheres loaded with Rg3 were prepared using a multi-step emulsification method and were characterized in vitro and in vivo.



The microspheres had a spherical shape with a mean diameter of 44.9±12.6 08m. The drugloading ratio was 10.25±0.08%, and the encapsulation ratio was 30.61±1.46%. Our in vitro mucoadhesion experiment demonstrated that 70.35±1.79% of the microspheres adhered to the nasal mucosa. The in vitro release study revealed that 31.1% of the Rg3 was released from the microspheres in the first 10 min. Release slowed, with 88.64% of the Rg3 released within 6 h. The pharmacodynamics study demonstrated that the weight-bearing swimming time of mice increased significantly from 432±89 s to 486±96 s after administration of Rg3 microspheres compared with the Rg3 water solution. Blood lactic acid and serum urea nitrogen significantly decreased in the group administered microspheres compared to the water solution group (p<0.05). Hepatic glycogen and lactate dehydrogenase increased significantly in the group administered microspheres compared to the water solution group (p<0.01).



20 (R) -ginsenoside Rg3 entrapped in chitosan microspheres may have a beneficial effect against fatigue by increasing the residence time of Rg3 in the nasal cavity and enhancing absorption by the nasal mucosa.
Department of Pharmacy, Shanghai Pulmonary Hospital, Tongji University School, Shanghai 200433, China
Wei
W
Zhang
Department of Pharmacy of the Second Military Medical University Changhai Hospital, Shanghai 200433, P.R. China
Xiaoyu
X
Wang
Department of Pharmacy of the Second Military Medical University Changhai Hospital, Shanghai 200433, P.R. China|Department of Pharmacy, Huadong Hospital affiliated to Fudan University , Shanghai 200040 , China
Min
M
Zhang
Department of Pharmaceutical Science of the Second Military Medical University School of Pharmacy, Shanghai 200433, P.R. China
Min
M
Xu
Department of Pharmaceutical Science of the Second Military Medical University School of Pharmacy, Shanghai 200433, P.R. China
Wenyan
W
Tang
Department of Pharmacy of the Second Military Medical University Changhai Hospital, Shanghai 200433, P.R. China
Yi
Y
Zhang
Department of Pharmacy of the Second Military Medical University Changhai Hospital, Shanghai 200433, P.R. China
Lei
L
Lu
Department of Pharmaceutical Science of the Second Military Medical University School of Pharmacy, Shanghai 200433, P.R. China|Institute of Pharmacology & Toxicology, Academy of Military Medical Science, Beijing 100850, P.R. China
Jing
J
Gao
Department of Pharmacy of the Second Military Medical University Changhai Hospital, Shanghai 200433, P.R. China|Department of Pharmaceutical Science of the Second Military Medical University School of Pharmacy, Shanghai 200433, P.R. China
Shen
S
Gao
D000281:Administration, Intranasal / Q000379:methods; D000818:Animals; D048271:Chitosan / Q000737:chemistry; D016503:Drug Delivery Systems / Q000379:methods; D005221:Fatigue / Q000188:drug therapy*; D005260:Female; D036145:Ginsenosides / Q000008:administration & dosage*; D008297:Male; D051379:Mice; D008863:Microspheres; D009297:Nasal Mucosa / Q000187:drug effects; D010316:Particle Size; D017207:Rats, Sprague-Dawley
D036145:Ginsenosides; C097367:ginsenoside Rg3; D048271:Chitosan
20 (R)-ginsenoside Rg3; Anti-fatigue; intranasal delivery; microspheres; nasal cavity; nasal mucosa