TY - JOUR
T1 - Engineering poly(lactic-co-glycolic acid) (PLGA) micro- and nano-carriers for Controlled Delivery of 17β-Estradiol
AU - Prakapenka, Alesia V.
AU - Bimonte-Nelson, Heather
AU - Sirianni, Rachael W.
N1 - Funding Information:
The authors would like to acknowledge the Barrow Neurological Institute and the ASU-BNI Interdepartmental Neuroscience Program. Dr. Rachael Sirianni and Alesia Prakapenka are funded by the NSF Graduate Research Fellowship. Dr. Heather Bimonte-Nelson is funded by NIA (AG028084), state of Arizona, and Arizona Department of Health Services (ADHS 14-052688).
Publisher Copyright:
© 2017, Biomedical Engineering Society.
PY - 2017/7/1
Y1 - 2017/7/1
N2 - With menopause, circulating levels of 17β-estradiol (E2) markedly decrease. E2-based hormone therapy is prescribed to alleviate symptoms associated with menopause. E2 is also recognized for its beneficial effects in the central nervous system (CNS), such as enhanced cognitive function following abrupt hormonal loss associated with ovariectomy. For women with an intact uterus, an opposing progestogen component is required to decrease the risk of developing endometrial hyperplasia. While adding an opposing progestogen attenuates these detrimental effects on the uterus, it can attenuate the beneficial effects of E2 in the CNS. Poly(lactic-co-glycolic acid) (PLGA) micro- and nano- carriers (MNCs) have been heavily investigated for their ability to enhance the therapeutic activity of hydrophobic agents following exogenous administration, including E2. Multiple PLGA MNC formulation parameters, such as composition, molecular weight, and type of solvent used, can be altered to systematically manipulate the pharmacokinetic and pharmacodynamic profiles of encapsulated agents. Thus, there is an opportunity to enhance the therapeutic activity of E2 in the CNS through controlled delivery from PLGA MNCs. The aim of this review is to consider the fate of exogenously administered E2 and discuss how PLGA MNCs and route of administration can be used as strategies for controlled E2 delivery.
AB - With menopause, circulating levels of 17β-estradiol (E2) markedly decrease. E2-based hormone therapy is prescribed to alleviate symptoms associated with menopause. E2 is also recognized for its beneficial effects in the central nervous system (CNS), such as enhanced cognitive function following abrupt hormonal loss associated with ovariectomy. For women with an intact uterus, an opposing progestogen component is required to decrease the risk of developing endometrial hyperplasia. While adding an opposing progestogen attenuates these detrimental effects on the uterus, it can attenuate the beneficial effects of E2 in the CNS. Poly(lactic-co-glycolic acid) (PLGA) micro- and nano- carriers (MNCs) have been heavily investigated for their ability to enhance the therapeutic activity of hydrophobic agents following exogenous administration, including E2. Multiple PLGA MNC formulation parameters, such as composition, molecular weight, and type of solvent used, can be altered to systematically manipulate the pharmacokinetic and pharmacodynamic profiles of encapsulated agents. Thus, there is an opportunity to enhance the therapeutic activity of E2 in the CNS through controlled delivery from PLGA MNCs. The aim of this review is to consider the fate of exogenously administered E2 and discuss how PLGA MNCs and route of administration can be used as strategies for controlled E2 delivery.
KW - 17β-Estradiol
KW - Cognition
KW - Drug delivery
KW - E2
KW - Microparticle
KW - Nanoparticle
KW - PLGA
KW - Polymer
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U2 - 10.1007/s10439-017-1859-8
DO - 10.1007/s10439-017-1859-8
M3 - Article
C2 - 28634732
AN - SCOPUS:85021169072
SN - 0090-6964
VL - 45
SP - 1697
EP - 1709
JO - Annals of Biomedical Engineering
JF - Annals of Biomedical Engineering
IS - 7
ER -