Formulation and Evaluation of a Self-Microemulsifying Drug Delivery System of Raloxifene with Improved Solubility and Oral Bioavailability

被引:8
|
作者
Ansari, Muhammad Mohsin [1 ]
Vo, Dang-Khoa [2 ]
Choi, Ho-Ik [3 ]
Ryu, Jeong-Su [3 ]
Bae, Yumi [3 ]
Bukhari, Nadeem Irfan [4 ]
Zeb, Alam [1 ,2 ]
Kim, Jin-Ki [3 ]
Maeng, Han-Joo [2 ]
机构
[1] Riphah Int Univ, Riphah Inst Pharmaceut Sci, Islamabad 44000, Pakistan
[2] Gachon Univ, Coll Pharm, 191 Hambakmoe Ro, Incheon 21936, South Korea
[3] Hanyang Univ, Inst Pharmaceut Sci & Technol, Coll Pharm, 55 Hanyangdaehak Ro, Ansan 15588, South Korea
[4] Punjab Univ Coll Pharm, Univ Punjab, Lahore 54590, Pakistan
基金
新加坡国家研究基金会;
关键词
raloxifene hydrochloride; BCS class II; solubility; dissolution; oral bioavailability; SMEDDS; ENHANCED INTESTINAL-ABSORPTION; SOLID DISPERSION; DESIGN; METABOLISM; OPTIMIZATION; DISSOLUTION; SMEDDS; RATS; PHARMACOKINETICS; HYDROCHLORIDE;
D O I
10.3390/pharmaceutics15082073
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
Poor aqueous solubility and dissolution limit the oral bioavailability of Biopharmaceutics Classification System (BCS) class II drugs. In this study, we aimed to improve the aqueous solubility and oral bioavailability of raloxifene hydrochloride (RLX), a BCS class II drug, using a self-microemulsifying drug delivery system (SMEDDS). Based on the solubilities of RLX, Capryol 90, Tween 80/Labrasol ALF, and polyethylene glycol 400 (PEG-400) were selected as the oil, surfactant mixture, and cosurfactant, respectively. Pseudo-ternary phase diagrams were constructed to determine the optimal composition (Capryol 90/Tween 80/Labrasol ALF/PEG-400 in 150/478.1/159.4/212.5 volume ratio) for RLX-SMEDDS with a small droplet size (147.1 nm) and stable microemulsification (PDI: 0.227). Differential scanning calorimetry and powder X-ray diffraction of lyophilized RLX-SMEDDS revealed the loss of crystallinity, suggesting a molecularly dissolved or amorphous state of RLX in the SMEDDS formulation. Moreover, RLX-SMEDDS exhibited significantly higher saturation solubility and dissolution rate in water, simulated gastric fluid (pH 1.2), and simulated intestinal fluid (pH 6.8) than RLX powder. Additionally, oral administration of RLX-SMEDDS to female rats resulted in 1.94- and 1.80-fold higher area under the curve and maximum plasma concentration, respectively, than the RLX dispersion. Collectively, our findings suggest SMEDDS is a promising oral formulation to enhance the therapeutic efficacy of RLX.
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页数:20
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