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Study on Bloven polyalkylcyanoacrylate nanoparticles for oral drug delivery system

Author: ChenYan
Tutor: ChenDaWei
School: Shenyang Pharmaceutical University
Course: Pharmacy
Keywords: Polyalkylcyanoacrylate Ibuprofen Nanoparticles Ether- interfacial polymerization method Oral administration Pharmacokinetics Tissue distribution
CLC: R94
Type: Master's thesis
Year: 2007
Downloads: 40
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Abstract

Polyalkylcyanoacrylate （PACA） is biodegradable as nanoparticles carrier. It have a lot of perfect property such as targeting in vivo, Sustained drug release, biological degradability, simple and convenient preparation method, low toxicity, high drug loading and so on. It is also one of minority carriers which can pass Blood-Brain barrier （BBB）. Therefore, more and more attention has been putting on PACA recently. In this thesis we have studied the preparation of PACA-NP, pharmacokinetics and tissue distribution with oral administration.Firstly, a HPLC method was developed to determine IBU in vitro, physical and chemical properties of IBU such as equilibrium solubility in various solutions and apparent oil-water partition coefficient were investigated.Ether-interfacial polymerization method was established to prepare IBU-PACA-NP on the basis of emulsion polymerization method and interfacial polymerization method. Separate free IBU and nanoparticles by ultraultracentrifugation and determine encapsulation efficiency（EE） and drug loading（DL） by HPLC. The EE and DL were used to evaluate the influence of different formulation and preparation factors. After the optimization of formulation by orthogonal design L₉ （3⁴）, the optimal formulation was obtained.The quality of IBU-PACA-NP suspension prepared by the optimal formulation was evaluated. IBU-PACA-NP was spheroidal shape through observing by transmission electron microscopy, the mean volume particle diameter was 166nm, the zeta potential was-31.7mv, the value of pH was close to 6.0, the amount of IBU was 1.48mg/mL, EE was 96.60%, DL wasl 7.83%, and it can be kept stable at room temperature for one month.The study using pH7.4 PBS as release medium to evaluate in vitro IBU release was carried on. From the results we observed a burst release at the beginning followed by a prolonged release. Weibull distribution was adopted to describe the release profiles.An HPLC method was developed for the determination of IBU in rat plasma. The study of pharmacokinetics of commercial IBU capsule and IBU-PACA-NP suspension in rats with oral administration showed the two preparations were both accorded with one-compartment model（W=1/C²）. Their eliminative half-life were 1.86h±0.13h、4.07h±0.66h, MRT were3.16h±0.32h、5.52h±0.48h, AUC_（0-14h） were 348.43μg·mL^-1·h、435.29μg·mL^-1·h respectively, and the relative bioavailability was 124.93％. The results indicated that the IBU-PACA-NP suspension eliminated slower and presented a prolonged release.A HPLC method was developed for the determination of IBU in rat tissue samples. The tissue distribution of commercial IBU capsule and IBU-PACA-NP suspension in rat with oral administration was investigated. The results showed that compared with commercial IBU capsule, in liver, lung, kidney, brain IBU-PACA-NP was distributed more quickly and eliminated slower; and at 5 points there was significant difference in liver, brain, spleen between two groups.

Study on Bloven polyalkylcyanoacrylate nanoparticles for oral drug delivery system

Abstract

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