Oral delivery of capsaicin using MPEG-PCL nanoparticles

Abstract

Aim: To prepare a biodegradable polymeric carrier for oral delivery of a water-insoluble drug capsaicin (CAP) and evaluate its quality. Methods: CAP-loaded methoxy poly (ethylene glycol)-poly(ε-caprolactone) nanoparticles (CAP/NPs) were prepared using a modified emulsification solvent diffusion technique. The quality of CAP/NPs were evaluated using transmission electron microscopy, powder X-ray diffraction, differential scanning calorimetry and Fourier transform infrared techniques. A dialysis method was used to analyze the in vitro release profile of CAP from the CAP/NPs. Adult male rats were orally administered CAP/NPs (35 mg/kg), and the plasma concentrations of CAP were measured with a validated HPLC method. The morphology of rat gastric mucosa was studied with HE staining. Results: CAP/NPs had an average diameter of 82.54±0.51 nm, high drug-loading capacity of 14.0%±0.13% and high stability. CAP/NPs showed a biphasic release profile in vitro: the burst release was less than 25% of the loaded drug within 12 h followed by a more sustained release for 60 h. The pharmacokinetics study showed that the mean maximum plasma concentration was observed 4 h after oral administered of CAP/NPs, and approximately 90 ng/mL of CAP was detected in serum after 36 h. The area under the curve for the CAP/NPs group was approximately 6-fold higher than that for raw CAP suspension. Histological studies showed that CAP/NPs markedly reduced CAP-caused gastric mucosa irritation. Conclusion: CAP/NPs significantly enhance the bioavailability of CAP and markedly reduce gastric mucosa irritation in rats.

A three-drug nanoscale drug delivery system designed for preferential lymphatic uptake for the treatment of metastatic melanoma

“…[49] Previous studies have demonstrated that solid state interactions between the drug and the hydrophobic block, and the mobility of the hydrophobic block all govern the drug release rate. [46] LY has the fastest drug release from the three-drug NP followed by DTX and then EVR. This may be due to the relative hydrophobicities of these molecules and their potential interaction with the PCL domain.…”

“…This biphasic release pattern exhibited by PEG-PCL NP has been well documented in the literature. [46,47] The initial burst release is primarily driven by the desorption and the diffusion of surface adsorbed drug particles, while the secondary phase of drug release is driven by the erosion of the NP matrix and drug diffusion processes. The inner segment, PCL, is a biodegradable polyester that has a high crystallinity while the outer PEG shell increases the porosity in the PCL matrix and thereby allows the diffusion of drugs from the matrix into the buffer.…”

Oral delivery of indinavir using mPEG-PCL nanoparticles: preparation, optimization, cellular uptake, transport and pharmacokinetic evaluation

“…According to the previous reports, mPEG-PCL copolymer has been synthesized by ring-opening polymerization of e-caprolactone, initiated by mPEG-5000 with Sn(Oct) 2 as a catalyst [26][27][28]. Briefly, pre-weighted amount of mPEG and e-caprolactone (w/w ¼ 1:2) were introduced into a dry twonecked flask containing Sn(Oct) 2 and then dissolved in an anhydrous toluene solution.…”

Encapsulation of clozapine into polycaprolactone nanoparticles as a promising strategy of the novel nanoformulation of the active compound

“…PCL NPs are characterized by a diameter lower than 100 nm and ability of passive targeting and sustained drug release (Kim et al 2015). What is more, over the last few years, a significant necessity emerged to evaluate PCL NPs possible pharmaceutical applications in drug delivery systems, due to their ability to transport variety of hydrophobic drugs and relatively lower cost of production and more satisfying biocompatibility (Peng et al 2015).…”