[Tetrandrine loaded sustained-release microcapsules for lung targeting].
OBJECTIVE
To prepare lung targeted tetrandrine (TET) loaded sustained-release drug delivery system by microencapsulation, decrease the toxicity and enhance the therapeutic function of anti-pulmonary hypertension of TET.


METHODS
Albumin microcapsules were produced by spray drying-thermal denaturation, a new technique. Some characterization of the prepared microcapsules was evaluated. Distribution of the microcapsules and their anti-pulmonary hypertension effect in vivo were investigated.


RESULTS
The spherical microcapsules showed a drug loading of 37.88%. Compared to the original drug, the rate of TET released from the positively charged microcapsules in vitro was significantly decreased and fitted well by Higuchi equation. The TET concentrations in mouse lungs of TET microcapsules were significantly higher than those of TET injection, and the mean retained time of TET in lungs was prolonged from 157.1 h to 223.6 h after microencapsulation. The in vitro--in vivo correlation was established and confirmed (P < 0.001).


CONCLUSIONS
The new spray drying-thermal denaturation method allows the preparation of drug loaded albumin microcapsules with desired results. The prepared microcapsules were found to have the potential function of delivering TET to pulmonary artery via i.v., with low toxicity and high efficacy.
Li
F Q
FQ
School of Pharmacy, West China University of Medical Sciences, Chengdu 610041, China.
Lu
B
B
Chen
W B
WB
Yang
H
H
D000470:Alkaloids / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000494:pharmacology; D000818:Animals; D000959:Antihypertensive Agents / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000494:pharmacology; D044182:Benzylisoquinolines; D001794:Blood Pressure / Q000187:drug effects; D002214:Capsules; D003692:Delayed-Action Preparations; D016503:Drug Delivery Systems; D004365:Drugs, Chinese Herbal / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000494:pharmacology; D006976:Hypertension, Pulmonary / Q000378:metabolism; D008168:Lung / Q000378:metabolism*; D051379:Mice; D011897:Random Allocation; D051381:Rats; D017208:Rats, Wistar; D014018:Tissue Distribution
D000470:Alkaloids; D000959:Antihypertensive Agents; D044182:Benzylisoquinolines; D002214:Capsules; D003692:Delayed-Action Preparations; D004365:Drugs, Chinese Herbal; C009438:tetrandrine