Cationic Solid SMEDDS of Efavirenz for Improved Oral Delivery: Development by Central Composite Design, In Vitro and In Vivo Evaluation

被引:4
作者
Thota, Sunil Kumar [1 ]
Dudhipala, Narendar [1 ]
Katla, Venumadhav [1 ]
Veerabrahma, Kishan [1 ,2 ]
机构
[1] Kakatiya Univ, Univ Coll Pharmaceut Sci, Dept Nanotechnol, Warangal 506009, Telangana, India
[2] Kakatiya Univ, Univ Coll Pharmaceut Sci, Dept Pharmaceut, Warangal 506009, Telangana, India
关键词
anti-HIV drug; bioavailability enhancement and central composite design; cationic solid SMEDDS; efavirenz; octadecylamine modified; LIPID NANOPARTICLES; SYSTEMS SEDDS; SELF; OPTIMIZATION; FORMULATION; DISSOLUTION; BIOAVAILABILITY; ABSORPTION;
D O I
10.1208/s12249-022-02495-3
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
Efavirenz (EFV) is an anti-HIV drug with high dose and 40% oral bioavailability (BA). The aim was to improve the bioavailability by designing cationic solid SMEDDS. Solubility data, ternary phase diagrams, and central composite design were employed in design. Globule size, TEM, DSC, and SEM studies were used for characterization. Optimized L-SMEDDS contained 20 mg of EFV, 10 mg of Peceol, 43.5 mg of Tween 80, and 40 mg of Labrafac Lipophile WL-1349 and the characters included mean globule size-94 nm, PDI-0.255, and ZP-28 mV. Later, octadecylamine was added to get L-SMEDDS with + 38 mV charge. L-SMEDDS was converted into solid S-SMEDDS by adsorbing onto silica carriers. Syloid XDP was preferred based on flow and oil adsorption capacity. The % drug (EFV) release from powder, L-SMEDDS, and solid SMEDDS were 14.04, 94.47, and 85 respectively in first 30 min. TEM picture showed dispersed globules. DSC and SEM studies indicated the loss of drug crystallinity in S-SMEDDS. Pharmacokinetic (PK) studies in Wistar rats revealed 4.12 fold hike in BA for optimized cationic S-SMEDDS when compared to EFV suspension. Increased absorption could be due to the positive charge on globules. Thus, cationic S-SMEDDS emerged as a potential novel delivery system for improvement in BA and has scope for reducing the high dose for AIDS patients by future clinical studies.
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页数:15
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