The in vivo transformation and pharmacokinetic properties of a liquid crystalline drug delivery system

[Display omitted] A liquid crystalline (LC) system, composed of phosphatidylcholine, sorbitan monoleate, and tocopherol acetate, was investigated to understand the in vivo transformation after subcutaneous injection, coupled with the physicochemical and pharmacokinetic properties of the formulation....

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Bibliographic Details
Published in:International journal of pharmaceutics 2017-10, Vol.532 (1), p.345-351
Main Authors: Otte, Andrew, Báez-Santos, Yahira M., Mun, Ellina A., Soh, Bong-Kwan, Lee, Young-nam, Park, Kinam
Format: Article
Language:English
Subjects:
alpha-Tocopherol - administration & dosage
alpha-Tocopherol - chemistry
alpha-Tocopherol - pharmacokinetics
Animals
Antineoplastic Agents, Hormonal - administration & dosage
Antineoplastic Agents, Hormonal - blood
Antineoplastic Agents, Hormonal - chemistry
Antineoplastic Agents, Hormonal - pharmacokinetics
Drug Delivery Systems
Drug Liberation
Fertility Agents, Female - administration & dosage
Fertility Agents, Female - blood
Fertility Agents, Female - chemistry
Fertility Agents, Female - pharmacokinetics
Hexagonal mesophase
Hexoses - administration & dosage
Hexoses - chemistry
Hexoses - pharmacokinetics
Injections, Subcutaneous
Leuprolide
Leuprolide - administration & dosage
Leuprolide - blood
Leuprolide - chemistry
Leuprolide - pharmacokinetics
Liquid crystal
Liquid Crystals - chemistry
Phosphatidylcholines - administration & dosage
Phosphatidylcholines - chemistry
Phosphatidylcholines - pharmacokinetics
Rats
Rheology
SAXS
Subcutaneous drug delivery
Sustained-release
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Summary:[Display omitted] A liquid crystalline (LC) system, composed of phosphatidylcholine, sorbitan monoleate, and tocopherol acetate, was investigated to understand the in vivo transformation after subcutaneous injection, coupled with the physicochemical and pharmacokinetic properties of the formulation. The rat model was utilized to monitor a pseudo-time course transformation from a precursor LC formulation to the LC matrix, coupled with the blood concentration profiles of the formulations containing leuprolide acetate. Three formulations that result in the HII phase, demonstrating dissimilar in vitro release profiles, were used. The formulation showing the highest AUC, Cmax and Tmax, also displayed the greatest release rate in vitro, the lowest viscosity (LC matrix), and an earlier transformation (LC precursor to matrix) in vivo. A potential link between viscosity, phase transformation, and drug release properties of a liquid crystalline system is described.
ISSN:0378-5173
1873-3476
DOI:10.1016/j.ijpharm.2017.08.098