Preparation of Puerarin Chitosan Oral Nanoparticles by Ionic Gelation Method and Its Related Kinetics

Abstract

In this paper, as an active ingredient, puerarin chitosan nanoparticles (Pur-CS/TPP-NPs) are prepared by an ionic gelation method. The chitosan (CS) concentration, pH of the CS solution, sodium tripolyphosphate (TPP) concentration, stirring speed, stirring time, ultrasonic power, and dosage are used as single factors for investigation, and the encapsulation efficiency, drug loading capacity, particle size, and polydispersity index (PDI) are used as indicators for investigation. The optimal prescription is determined using the Box–Behnken effect surface design method. The characterization of the best formulation, which is determined via an in vitro release assay and liquid chromatography/tandem mass spectrometry (LC-MS/MS) analysis methods, is used here for pharmacokinetic studies. An in situ single-pass intestinal perfusion model is used to investigate drug absorption in the intestine. After characterization, the morphologies of the nanoparticles are intact. It can be seen from the in vitro release experiments that the equation fitted by the nanoparticles is the Higuchi model, the nanoparticle release process is very stable and without sudden release, indicating that the nanoparticles are well-released in vitro. The pharmacokinetic results and the in situ single-pass intestinal perfusion model study show that the bioavailability and absorption of Pur-CS/TPP-NPs were significantly higher than Pur. Thus, all the results show that the prepared nanoparticles can significantly improve the bioavailability of Pur, and we hope to lay the foundation for the development of new products of Pur.

Ionotropic Gelation of Chitosan Flat Structures and Potential Applications

“…The cellular uptake of molecules encapsulated in 200 nm chitosan nanoparticles, at 24 h, was observed in the case of the anticancer agent resveratrol [168] and BSA [3]. Similar in vivo results in a single-pass intestinal perfusion model were observed for puerarin (a molecule with bioprotective activity and obtained from a leguminous plant), which increased its bioavailability by a factor of 4.4 when encapsulated in chitosan nanoparticles [169]. Other approaches include the synthesis of thermo-responsive structures [2] and micro/nanoparticles [170,171] encapsulating the chemotherapeutic (anticancer agent) doxorubicin; and the combination of a chemotherapy (5-fluorouracil) with magnetic nanoparticles to obtain a core-shell structure for drug delivery and hyperthermia therapy [172].…”

Encapsulation of the Natural Product Tyrosol in Carbohydrate Nanosystems and Study of Their Binding with ctDNA

“…The high ζ-potential of those points confirms the existence of protonated amino groups on the surface of the NPs. Moreover, increased concentration of chitosan leads in decreased intermolecular distance and increased intermolecular hydrogen bonding between the polymeric chains [ 30 , 31 , 32 , 33 , 34 ].…”

Reverse genetic systems: Rational design of coronavirus live attenuated vaccines with immune sequelae

“…The best-known examples include SARS-CoV, MERS-CoV and SARS-CoV-2 (Chan et al, 2020), all of which pose a marked threat to human health. In addition, four other coronaviruses are known to infect humans, including HCoV-229E, HKU-NL63, HCoV-OC43 and HCoV-HKU1, which cause mild illnesses (Li et al, 2020a;Yan et al, 2020). Bats are generally thought to be the natural reservoir of a range of coronaviruses (Graham et al, 2013).…”

“…In early December 2019, a cluster of cases of pneumonia caused by a novel coronavirus named Sudden Acute Respiratory Syndrome Coronavirus 2 (SARS-CoV-2) resulted in tremendous challenges to China's public health and clinical treatment (Munster et al, 2020;Yan et al, 2020), and now it has been confirmed in more than 211 other countries and territories, causing a major global public health crisis (Day, 2020;Jernigan and Team, 2020;Peeri et al, 2020). SARS-CoV-2 belongs to the Betacoronavirus genus in the family Coronaviridae, and is closely related to severe acute respiratory syndrome coronavirus (SARS-CoV) and Middle East respiratory syndrome coronavirus (MERS-CoV) (Drosten et al, 2003;Wassenaar and Zou, 2020;Zaki et al, 2012).…”