PMID- 28119812
OWN - NLM
STAT- PubMed-not-MEDLINE
LR  - 20240324
IS  - 2211-3835 (Print)
IS  - 2211-3843 (Electronic)
IS  - 2211-3835 (Linking)
VI  - 7
IP  - 1
DP  - 2017 Jan
TI  - Inhalable oridonin-loaded poly(lactic-co-glycolic)acid large porous 
      microparticles for in situ treatment of primary non-small cell lung cancer.
PG  - 80-90
LID - 10.1016/j.apsb.2016.09.006 [doi]
AB  - Non-small cell lung cancer (NSCLC) accounts for about 85% of all lung cancers. 
      Traditional chemotherapy for this disease leads to serious side effects. Here we 
      prepared an inhalable oridonin-loaded poly(lactic-co-glycolic)acid (PLGA) large 
      porous microparticle (LPMP) for in situ treatment of NSCLC with the 
      emulsion/solvent evaporation/freeze-drying method. The LPMPs were smooth spheres 
      with many internal pores. Despite a geometric diameter of ~10 microm, the aerodynamic 
      diameter of the spheres was only 2.72 microm, leading to highly efficient lung 
      deposition. In vitro studies showed that most of oridonin was released after 1 h, 
      whereas the alveolar macrophage uptake of LPMPs occurred after 8 h, so that most 
      of oridonin would enter the surroundings without undergoing phagocytosis. Rat 
      primary NSCLC models were built and administered with saline, oridonin powder, 
      gemcitabine, and oridonin-loaded LPMPs via airway, respectively. The LPMPs showed 
      strong anticancer effects. Oridonin showed strong angiogenesis inhibition and 
      apoptosis. Relevant mechanisms are thought to include oridonin-induced 
      mitochondrial dysfunction accompanied by low mitochondrial membrane potentials, 
      downregulation of BCL-2 expressions, upregulation of expressions of BAX, 
      caspase-3 and caspase-9. The oridonin-loaded PLGA LPMPs showed high anti-NSCLC 
      effects after pulmonary delivery. In conclusion, LPMPs are promising dry powder 
      inhalations for in situ treatment of lung cancer.
FAU - Zhu, Lifei
AU  - Zhu L
AD  - Department of Pharmaceutical Sciences, Beijing Institute of Radiation Medicine, 
      Beijing 100850, China; Anhui Medical University, Hefei 230001, China; Department 
      of Pharmacy, Yangpu Hospital, Tongji University School of Medicine, Shanghai 
      200090, China.
FAU - Li, Miao
AU  - Li M
AD  - Department of Pharmaceutical Sciences, Beijing Institute of Radiation Medicine, 
      Beijing 100850, China.
FAU - Liu, Xiaoyan
AU  - Liu X
AD  - Department of Pharmaceutical Sciences, Beijing Institute of Radiation Medicine, 
      Beijing 100850, China.
FAU - Du, Lina
AU  - Du L
AD  - Department of Pharmaceutical Sciences, Beijing Institute of Radiation Medicine, 
      Beijing 100850, China.
FAU - Jin, Yiguang
AU  - Jin Y
AD  - Department of Pharmaceutical Sciences, Beijing Institute of Radiation Medicine, 
      Beijing 100850, China; Anhui Medical University, Hefei 230001, China.
LA  - eng
PT  - Journal Article
DEP - 20161222
PL  - Netherlands
TA  - Acta Pharm Sin B
JT  - Acta pharmaceutica Sinica. B
JID - 101600560
PMC - PMC5237759
OTO - NOTNLM
OT  - BSA, bovine serum albumin
OT  - DAB, 3,3'-diaminobenzidine
OT  - DAPI, 4',6-diamidino-2-phenylindole
OT  - DPI, dry powder inhalation
OT  - EGFR, epidermal growth factor receptor
OT  - FPF, fine particle fraction
OT  - HPLC, high performance liquid chromatography
OT  - HRP, horseradish peroxidase
OT  - LPMP, large porous microparticle
OT  - Large porous microparticle
OT  - NSCLC, non-small cell lung cancer
OT  - Non-small cell lung cancer
OT  - Oridonin
OT  - PLGA, poly(lactic-co-glycolic)acid
OT  - PVA, polyvinyl alcohol
OT  - Poly(lactic-co-glycolic)acid
OT  - Pulmonary delivery
OT  - SEM, scanning electron microscopy
OT  - SLF, simulated lung fluid
OT  - TCM, traditional Chinese medicine
OT  - XRD, X-ray diffraction
OT  - qPCR, quantitative polymerase chain reaction
EDAT- 2017/01/26 06:00
MHDA- 2017/01/26 06:01
PMCR- 2016/12/22
CRDT- 2017/01/26 06:00
PHST- 2016/06/03 00:00 [received]
PHST- 2016/08/16 00:00 [revised]
PHST- 2016/08/23 00:00 [accepted]
PHST- 2017/01/26 06:00 [entrez]
PHST- 2017/01/26 06:00 [pubmed]
PHST- 2017/01/26 06:01 [medline]
PHST- 2016/12/22 00:00 [pmc-release]
AID - S2211-3835(16)30193-9 [pii]
AID - 10.1016/j.apsb.2016.09.006 [doi]
PST - ppublish
SO  - Acta Pharm Sin B. 2017 Jan;7(1):80-90. doi: 10.1016/j.apsb.2016.09.006. Epub 2016 
      Dec 22.