Phospholipid-based complex of raloxifene with enhanced biopharmaceutical potential: Synthesis, characterization and preclinical assessment

Jain, Atul; Saini, Sumant; Kumar, Rajendra; Sharma, Teenu; Swami, Rajan; Katare, Om Prakash; Singh, Bhupinder

doi:10.1016/j.ijpharm.2019.118698

Cited by 11 publications

(1 citation statement)

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“…Improving the solubility and dissolution rate of RLX will overcome its poor oral absorption. Various formulations, including lecithin–chitosan nanoparticles [ 15 ], solid dispersion [ 16 , 17 ], inclusion complexes [ 18 ], micro- and nano-emulsions [ 14 , 19 ], nanostructured lipid carriers [ 20 , 21 ], dry suspensions [ 22 ], mesoporous silica nanoparticles [ 23 ], phospholipid complexes [ 24 ], and polymeric nanoparticles [ 25 , 26 ], have been investigated to enhance the solubility and oral bioavailability of RLX. However, oral absorption of RLX remains low and continued efforts are required to improve its oral bioavailability.…”

Section: Introductionmentioning

confidence: 99%

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

Ansari

Choi

et al. 2023

Pharmaceutics

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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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