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Preparation and in vitro/in vivo evaluation of andrographolide nano-structured lipid carrier eye drops
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DOI   10.11656/j.issn.1673-9043.2026.09.06
Key Words   andrographolide;nanostructured lipid carrier;microdialysis pharmacokinetics;tissue distribution
Author NameAffiliationE-mail
CHEN Yanan School of Chinese Materia Medica, Tianjin University of Traditional Chinese Medicine, Tianjin 301617, China
Engineering Research Center of Modern Chinese Medicine Discovery and Preparation Technique, Ministry of Education, Tianjin 301617, China
State Key Laboratory of Component-based Chinese Medicine, Tianjin 301617, China 
 
LIN Yun School of Chinese Materia Medica, Tianjin University of Traditional Chinese Medicine, Tianjin 301617, China
Engineering Research Center of Modern Chinese Medicine Discovery and Preparation Technique, Ministry of Education, Tianjin 301617, China
State Key Laboratory of Component-based Chinese Medicine, Tianjin 301617, China 
 
ZHAO Mengfei School of Chinese Materia Medica, Tianjin University of Traditional Chinese Medicine, Tianjin 301617, China
Engineering Research Center of Modern Chinese Medicine Discovery and Preparation Technique, Ministry of Education, Tianjin 301617, China
State Key Laboratory of Component-based Chinese Medicine, Tianjin 301617, China 
 
LIU Yanling School of Chinese Materia Medica, Tianjin University of Traditional Chinese Medicine, Tianjin 301617, China
Engineering Research Center of Modern Chinese Medicine Discovery and Preparation Technique, Ministry of Education, Tianjin 301617, China
State Key Laboratory of Component-based Chinese Medicine, Tianjin 301617, China 
 
XIE Haonan School of Chinese Materia Medica, Tianjin University of Traditional Chinese Medicine, Tianjin 301617, China
Engineering Research Center of Modern Chinese Medicine Discovery and Preparation Technique, Ministry of Education, Tianjin 301617, China
State Key Laboratory of Component-based Chinese Medicine, Tianjin 301617, China 
 
DENG Xiuping Engineering Research Center of Modern Chinese Medicine Discovery and Preparation Technique, Ministry of Education, Tianjin 301617, China
State Key Laboratory of Component-based Chinese Medicine, Tianjin 301617, China 
 
LI Jiawei School of Chinese Materia Medica, Tianjin University of Traditional Chinese Medicine, Tianjin 301617, China
Engineering Research Center of Modern Chinese Medicine Discovery and Preparation Technique, Ministry of Education, Tianjin 301617, China
State Key Laboratory of Component-based Chinese Medicine, Tianjin 301617, China 
lijiawei1981@163.com 
LIU Zhidong School of Chinese Materia Medica, Tianjin University of Traditional Chinese Medicine, Tianjin 301617, China
Engineering Research Center of Modern Chinese Medicine Discovery and Preparation Technique, Ministry of Education, Tianjin 301617, China
State Key Laboratory of Component-based Chinese Medicine, Tianjin 301617, China 
lonerliuzd@163.com 
Abstract
    [Objective] To prepare Andrographolide-loaded nanostructured lipid carrier(AG-NLC) eye drops and evaluate them in vitro and in vivo. [Methods] In this study,AG-NLCs were prepared using the solvent injection method. Their encapsulation efficiency,drug loading,particle size,and zeta potential were determined. Morphology was observed using transmission electron microscopy. In vitro release and ex vivo corneal permeation studies were conducted using Andrographolide ophthalmic gel(AG-Gel) and an andrographolide API suspension(AG) as reference formulations,in vivo microdialysis kinetics and tissue distribution studies in rabbit eyes. [Results] The encapsulation efficiency of AG-NLCs was(79.98±0.75)%,drug loading was(0.36±0.03)%,particle size was(15.64±0.97) nm,the polydispersity index(PDI) was(0.193±0.013),the zeta potential was(1.05±0.00) mV,and the particles appeared as uniform spherical particles under electron microscopy. The in vitro release rates of AG-NLCs and AG-Gel were significantly superior to those of AG;the cumulative drug permeation at 3 h for AG-NLCs and AG-Gel was 6.18 times(P<0.01) and 4.69 times(P<0.05) that of AG,respectively;The apparent permeability coefficients(Papp) of AG-NLCs were 7.27 times that of AG-Gel(P<0.01) and 13.55 times that of AG(P<0.01);Following administration of AG-NLCs,the AUC0-8 values were 2.49 times(P<0.05) that of AG-Gel and 5.21 times(P<0.01) that of AG,and AG-NLCs demonstrated greater tissue retention capacity. [Conclusion] Compared with the reference formulation,the use of nanostructured lipid carrier eye drops can improve the ocular bioavailability of andrographolide.

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