Formulation of ciprofloxacin-loaded oral self-emulsifying drug delivery system to improve the pharmacokinetics and antibacterial activity

被引:10
作者
Asghar, Asghar Ali [1 ]
Akhlaq, Muhammad [1 ]
Jalil, Aamir [2 ]
Azad, Abul Kalam [3 ]
Asghar, Junaid [1 ]
Adeel, Muhammad [4 ]
Albadrani, Ghadeer M. [5 ]
Al-Doaiss, Amin A. [6 ]
Kamel, Mohamed [7 ]
Altyar, Ahmed E. [8 ]
Abdel-Daim, Mohamed M. [9 ,10 ]
机构
[1] Gomal Univ, Fac Pharm, Dera Ismail Khan, Pakistan
[2] Bahauddin Zakaria Univ, Fac Pharm, Dept Pharmaceut, Multan, Punjab, Pakistan
[3] MAHSA Univ, Fac Pharm, Jenjarom, Malaysia
[4] Gomal Univ, Inst Chem Sci, Dera Ismail Khan, Pakistan
[5] Princess Nourah Bint Abdulrahman Univ, Coll Sci, Dept Biol, Riyadh, Saudi Arabia
[6] King Khalid Univ, Fac Sci, Biol Dept, Abha, Saudi Arabia
[7] Cairo Univ, Fac Vet Med, Dept Med & Infect Dis, Giza, Egypt
[8] King Abdulaziz Univ, Fac Pharm, Dept Pharm Practice, Jeddah, Saudi Arabia
[9] Batterjee Med Coll, Dept Pharmaceut Sci, Pharm Program, Jeddah, Saudi Arabia
[10] Suez Canal Univ, Fac Vet Med, Pharmacol Dept, Ismailia, Egypt
关键词
ciprofloxacin; pseudo-ternary phase diagram; self-emulsifying drug delivery system; oral bioavailability; solubility; IN-VITRO CHARACTERIZATION; DESIGN; BIOAVAILABILITY; HYBRIDS;
D O I
10.3389/fphar.2022.967106
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
This study aims to increase the aqueous solubility of ciprofloxacin (CPN) to improve oral bioavailability. This was carried out by formulating a stable formulation of the Self-Emulsifying Drug Delivery System (SEDDS) using various ratios of lipid/oil, surfactant, and co-surfactant. A pseudo-ternary phase diagram was designed to find an area of emulsification. Eight formulations (F1-CPN-F8-CPN) containing oleic acid oil, silicone oil, olive oil, castor oil, sunflower oil, myglol oil, polysorbate-80, polysorbate-20, PEO-200, PEO-400, PEO-600, and PG were formulated. The resultant SEDDS were subjected to thermodynamic study, size, and surface charge studies to improve preparation. Improved composition of SEDDS F5-CPN containing 40% oil, 60% polysorbate-80, and propylene glycol (Smix ratio 6: 1) were thermodynamically stable emulsions having droplet size 202.6 nm, charge surface -13.9 mV, and 0.226 polydispersity index (PDI). Fourier transform infra-red (FT-IR) studies revealed that the optimized formulation and drug showed no interactions. Scanning electron microscope tests showed the droplets have an even surface and spherical shape. It was observed that within 5 h, the concentration of released CPN from optimized formulations F5-CPN was 93%. F5-CPN also showed a higher antibacterial action against S. aurous than free CPN. It shows that F5-CPN is a better formulation with a good release and high antibacterial activity.
引用
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页数:14
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