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Current Status of Supersaturable Self-Emulsifying Drug Delivery Systems
Article

Development and Evaluation of Docetaxel-Phospholipid Complex Loaded Self-Microemulsifying Drug Delivery System: Optimization and In Vitro/Ex Vivo Studies

1
College of Pharmacy and Institute of Drug Research and Development, Chungnam National University, 99, Daehak-ro, Yuseong-gu, Daejeon 34134, Korea
2
Hanall Biopharma Co. Ltd., 199 Techno 2-ro, Yuseong-gu, Daejeon 34025, Korea
*
Authors to whom correspondence should be addressed.
These authors contributed equally to this work.
Pharmaceutics 2020, 12(6), 544; https://doi.org/10.3390/pharmaceutics12060544
Received: 5 May 2020 / Revised: 10 June 2020 / Accepted: 11 June 2020 / Published: 12 June 2020
(This article belongs to the Special Issue Self-Emulsifying Drug Delivery System)
Docetaxel (DTX) has clinical efficacy in the treatment of breast cancer, but it is difficult to develop a product for oral administration, due to low solubility and permeability. This study focused on preparing a self-microemulsifying drug delivery system (SME) loaded with DTX-phospholipid complex ([email protected]), to improve the dissolution and gastrointestinal (GI) permeability of DTX. A dual technique combining the phospholipid complexation and SME formulation described as improving upon the disadvantages of DTX has been proposed. We hypothesized that the complexation of DTX with phospholipids can improve the lipophilicity of DTX, thereby increasing the affinity of the drug to the cell lipid membrane, and simultaneously improving permeability through the GI barrier. Meanwhile, [email protected] SME ([email protected]) increases the dissolution and surface area of DTX by forming a microemulsion in the intestinal fluid, providing sufficient opportunity for the drug to contact the GI membrane. First, we prepared [email protected] by combining dual technologies, which are advantages for oral absorption. Next, we optimized [email protected] with nanosized droplets (117.1 nm), low precipitation (8.9%), and high solubility (33.0 mg/g), which formed a homogeneous microemulsion in the aqueous phase. Dissolution and cellular uptake studies demonstrated that [email protected] showed 5.6-fold higher dissolution and 2.3-fold higher DTX uptake in Caco-2 cells than raw material. In addition, an ex vivo gut sac study confirmed that [email protected] improved GI permeability of DTX by 2.6-fold compared to raw material. These results suggested that [email protected] can significantly overcome the disadvantages of anticancer agents, such as low solubility and permeability. View Full-Text
Keywords: docetaxel; phospholipid complex; self-microemulsifying drug delivery system; dissolution; cell uptake; permeability docetaxel; phospholipid complex; self-microemulsifying drug delivery system; dissolution; cell uptake; permeability
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MDPI and ACS Style

Wang, M.; You, S.-K.; Lee, H.-K.; Han, M.-G.; Lee, H.-M.; Pham, T.M.A.; Na, Y.-G.; Cho, C.-W. Development and Evaluation of Docetaxel-Phospholipid Complex Loaded Self-Microemulsifying Drug Delivery System: Optimization and In Vitro/Ex Vivo Studies. Pharmaceutics 2020, 12, 544. https://doi.org/10.3390/pharmaceutics12060544

AMA Style

Wang M, You S-K, Lee H-K, Han M-G, Lee H-M, Pham TMA, Na Y-G, Cho C-W. Development and Evaluation of Docetaxel-Phospholipid Complex Loaded Self-Microemulsifying Drug Delivery System: Optimization and In Vitro/Ex Vivo Studies. Pharmaceutics. 2020; 12(6):544. https://doi.org/10.3390/pharmaceutics12060544

Chicago/Turabian Style

Wang, Miao, Sung-Kyun You, Hong-Ki Lee, Min-Gu Han, Hyeon-Min Lee, Thi M.A. Pham, Young-Guk Na, and Cheong-Weon Cho. 2020. "Development and Evaluation of Docetaxel-Phospholipid Complex Loaded Self-Microemulsifying Drug Delivery System: Optimization and In Vitro/Ex Vivo Studies" Pharmaceutics 12, no. 6: 544. https://doi.org/10.3390/pharmaceutics12060544

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