Evaluation of Lipid-based Drug Delivery System (Phytosolve) on Oral Bioavailability of Dibudipine

Overview

Journal Iran J Pharm Res

Publisher Brieflands

Specialty Pharmacology

Date 2015 Jan 15

PMID 25587302

Citations 2

Authors

Fariborz Keyhanfar

Samira Khani

Shahab Bohlooli

Affiliations

Soon will be listed here.

Abstract

The objective of present study was to evaluate pharmacokinetic parameters of dibudipine Phytosolve after oral administration in rats. The solubility test was carried out to select suitable oily solvent for dibudipine. Phytosolve formulation was prepared with a medium chain triglyceride (MCT) oil (20%), soybean phospholipids (5%) and a 70% fructose solution (75%). The effect of polyol content on the mean globule size of Phytosolve formulation was studied. The optimized formulation was evaluated for robustness toward dilution, transparency, droplet size, zeta potential and transmission electron microscopic analysis. The Phytosolve of dibudipine with an average droplet size of 142.3 ± 4.3 nm and surface charge -18.36 ± 0.37 mv was administered orally to rats. The average relative bioavalabilities of dibudipine in the plasma with Phytosolve were 170.4% and 211.2% as compared to the oily solution and aqueous suspension respectively. So this formulation could be offered as a useful technique to improve the oral delivery of the poorly water soluble drugs such as dibudipine.

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References

Hadian Z, Sahari M, Moghimi H, Barzegar M . Formulation, characterization and optimization of liposomes containing eicosapentaenoic and docosahexaenoic acids; a methodology approach. Iran J Pharm Res. 2014; 13(2):393-404. PMC: 4157015. View

Bohlooli S, Keyhanfar F, Ghiaee S, Mahmoudian M . Application of a new high performance liquid chromatography method to the pharmacokinetics of dibudipine in rats. J Pharm Pharm Sci. 2004; 6(3):346-51. View

Mirkhani H, Omrani G, Ghiaee S, Mahmoudian M . Effects of mebudipine and dibudipine, two new calcium-channel blockers, on rat left atrium, rat blood pressure and human internal mammary artery. J Pharm Pharmacol. 1999; 51(5):617-22. DOI: 10.1211/0022357991772727. View

Gannu R, Palem C, Yamsani V, Yamsani S, Rao Yamsani M . Enhanced bioavailability of lacidipine via microemulsion based transdermal gels: formulation optimization, ex vivo and in vivo characterization. Int J Pharm. 2010; 388(1-2):231-41. DOI: 10.1016/j.ijpharm.2009.12.050. View

Gershanik T, Benita S . Self-dispersing lipid formulations for improving oral absorption of lipophilic drugs. Eur J Pharm Biopharm. 2000; 50(1):179-88. DOI: 10.1016/s0939-6411(00)00089-8. View

Sun C, Wang J, Liu J, Qiu L, Zhang W, Zhang L . Liquid proliposomes of nimodipine drug delivery system: preparation, characterization, and pharmacokinetics. AAPS PharmSciTech. 2013; 14(1):332-8. PMC: 3581684. DOI: 10.1208/s12249-013-9924-6. View

Bunjes H . Lipid nanoparticles for the delivery of poorly water-soluble drugs. J Pharm Pharmacol. 2010; 62(11):1637-45. DOI: 10.1111/j.2042-7158.2010.01024.x. View

Trevaskis N, Porter C, Charman W . The lymph lipid precursor pool is a key determinant of intestinal lymphatic drug transport. J Pharmacol Exp Ther. 2005; 316(2):881-91. DOI: 10.1124/jpet.105.094094. View

Choi H, Kim D, Jun H, Yoo B, Yong C . Improvement of dissolution and bioavailability of nitrendipine by inclusion in hydroxypropyl-beta-cyclodextrin. Drug Dev Ind Pharm. 2003; 29(10):1085-94. DOI: 10.1081/ddc-120025866. View

10.

Stuchlik M, Zak S . Lipid-based vehicle for oral drug delivery. Biomed Pap Med Fac Univ Palacky Olomouc Czech Repub. 2002; 145(2):17-26. View

11.

Shah A, Agnihotri S . Recent advances and novel strategies in pre-clinical formulation development: an overview. J Control Release. 2011; 156(3):281-96. DOI: 10.1016/j.jconrel.2011.07.003. View

12.

Lawrence M, Rees G . Microemulsion-based media as novel drug delivery systems. Adv Drug Deliv Rev. 2000; 45(1):89-121. DOI: 10.1016/s0169-409x(00)00103-4. View

13.

Wajda R, Zirkel J, Schaffer T . Increase of bioavailability of coenzyme Q(10) and vitamin E. J Med Food. 2007; 10(4):731-4. DOI: 10.1089/jmf.2006.254. View

14.

Moreno M, Ballesteros M, Frutos P . Lecithin-based oil-in-water microemulsions for parenteral use: pseudoternary phase diagrams, characterization and toxicity studies. J Pharm Sci. 2003; 92(7):1428-37. DOI: 10.1002/jps.10412. View

15.

Thrivikraman K, Huot R, Plotsky P . Jugular vein catheterization for repeated blood sampling in the unrestrained conscious rat. Brain Res Brain Res Protoc. 2002; 10(2):84-94. DOI: 10.1016/s1385-299x(02)00185-x. View

16.

Bohlooli S, Mahmoudian M, Skellern G, Grant M, Tettey J . Metabolism of the dihydropyridine calcium channel blockers mebudipine and dibudipine by isolated rat hepatocytes. J Pharm Pharmacol. 2004; 56(11):1469-75. DOI: 10.1211/0022357044760. View

17.

Mahmoudian M, Mirkhani H, Nehardani Z, Ghiaee S . Synthesis and biological activity of two new calcium-channel blockers, mebudipine and dibudipine. J Pharm Pharmacol. 1998; 49(12):1229-33. DOI: 10.1111/j.2042-7158.1997.tb06075.x. View

18.

MakhmalZadeh B, Torabi S, Azarpanah A . Optimization of Ibuprofen Delivery through Rat Skin from Traditional and Novel Nanoemulsion Formulations. Iran J Pharm Res. 2014; 11(1):47-58. PMC: 3876571. View