10.1021/acs.jmedchem.5b00714.s002
Yan-Jye Shyong
Yan-Jye
Shyong
Mao-Hsien Wang
Mao-Hsien
Wang
Hsiang-Chien Tseng
Hsiang-Chien
Tseng
Chen Cheng
Chen
Cheng
Kuo-Chi Chang
Kuo-Chi
Chang
Feng-Huei Lin
Feng-Huei
Lin
Mesoporous Hydroxyapatite
as Olanzapine Carrier Provides
a Long-Acting Effect in Antidepression Treatment
American Chemical Society
2015
medication release
calcium ion
coprecipitation method
extracellular space
nonadherent medication intake
Mesoporous Hydroxyapatite
mesoHAP
Olanzapine Carrier Provides
Mesoporous hydroxyapatite
blood circulation
OLZ
2 weeks
drug release
treatment strategy
IM
surface modifications
antidepressant therapy
Antidepression TreatmentAn antidepressant carrier
2015-11-12 00:00:00
Dataset
https://acs.figshare.com/articles/dataset/Mesoporous_Hydroxyapatite_as_Olanzapine_Carrier_Provides_a_Long_Acting_Effect_in_Antidepression_Treatment/2109172
An
antidepressant carrier was designed to maintain over 2 weeks
of constant medication release. The carrier was injected into muscle,
where cellular activity was employed to achieve the goal of constant
release. Mesoporous hydroxyapatite (mesoHAP) was synthesized into
an adequate size by a coprecipitation method; it then went through
a series of hydrophobic surface modifications for olanzapine (OLZ)
loading by physical absorption to produce mesoHAP–OLZ. Because
of its hydrophobic nature, OLZ was not effectively released from mesoHAP–OLZ
in an aqueous environment. However, once engulfed by macrophages,
the lysosome/endosome hybrid ruptured due to alterations in osmotic
pressure, resulting in the release of OLZ into the cytoplasm. OLZ
was then exocytosed to the extracellular space due to a high calcium
ion (Ca<sup>2+</sup>) concentration and finally reached the blood
circulation. Our findings provide a useful treatment strategy to achieve
long-term drug release with a single intramuscular (IM) injection,
helping to solve the problem of nonadherent medication intake that
often occurs in antidepressant therapy.