Multi-ion-crosslinked nanoparticles with pH-responsive characteristics for oral delivery of protein drugs

Lin, Yu Hsin; Sonaje, Kiran; Lin, Kurt M.; Juang, Jyuhn Huarng; Mi, Fwu Long; Yang, Han Wen; Sung, Hsing‐Wen

doi:10.1016/j.jconrel.2008.08.020

Cited by 182 publications

(126 citation statements)

References 38 publications

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“…This result was in agreement with the transport study that FQS modified NPs possessed the optimal ability of transepithelial transport. Additionally, it worth to be noticed that a gradual recovery in TEER values was observed after the incubated test samples were removed ( Figure 5C), which is similar with former study that TEER values were reach 80% of initial after removing the chitosan NPs (Lin et al, 2008). These observations suggest that the T-NPs and FQS-NPs could open the TJs of Caco-2 cell monolayers reversibly and facilitate the permeation of insulin across intestinal epithelium.…”

Section: In Vitro Transport Studysupporting

confidence: 88%

A novel ligand conjugated nanoparticles for oral insulin delivery

et al. 2015

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In order to enhance the interaction between nanocarrier and gastrointestinal epithelial cells, we developed nanoparticles (NPs) modified with targeting ligand FQSIYPpIK (FQS), which specifically interact with integrin avb3 receptor expressing on the intestinal epithelium. The targeting NPs were prepared by coating the insulin-loaded poly(lactide-co-glycolide)-monomethoxy-poly(polyethylene glycol) micelle cores with FQS modified trimethyl chitosan chloride. In in vitro study, the fabricated NPs showed ameliorated drug release profile and improved enzymatic stability compared with micelles alone. In the integrin avb3 receptor over-expressed Caco-2 cells model, FQS modified NPs exhibited significantly accelerated intracellular uptake due to the active ligand-receptor mediation. Meanwhile, the targeting NPs also showed enhanced transport across the Caco-2 monolayer cells via both transcellular and paracellular pathways. Besides, orally administered FQS modified NPs produced a prominent hypoglycemic response and an increase of the serum insulin concentration in diabetic rats. Both in vitro and in vivo results demonstrated the FQS peptide modified NPs as promising intestinal cell-targeting nanocarriers for efficient oral delivery of insulin.

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Section: In Vitro Transport Studysupporting

confidence: 88%

A novel ligand conjugated nanoparticles for oral insulin delivery

et al. 2015

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“…Comparing with CS/g-PGA nanoparticles, the multiion-cross-linked nanoparticles could retain more insulin. With the addition of MgSO 4 and TPP, the cumulative amount of insulin released were significantly reduced at pH 2.5 and pH 7.0, while a fast release of insulin was observed at pH 7.4 (simulating the pH in the body fluid at intercellular spaces), which means insulin were more likely to be released from the multi-ion-cross-linked nanoparticles after they were infiltrated into mucus layer (Lin et al, 2008). Since SC injection of insulin often produces peripheral hyperinsulinemia in individuals.…”

Section: G-pga-based Materialsmentioning

confidence: 98%

A review of biodegradable polymeric systems for oral insulin delivery

Luo

Xiong

Tian³

et al. 2015

Drug Delivery

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Currently, repeated routine subcutaneous injections of insulin are the standard treatment for insulin-dependent diabetic patients. However, patients' poor compliance for injections often fails to achieve the stable concentration of blood glucose. As a protein drug, the oral bioavailability of insulin is low due to many physiological reasons. Several carriers, such as macromolecules and liposomes have been used to deliver drugs in vivo. In this review article, the gastrointestinal barriers of oral insulin administration are described. Strategies for increasing the bioavailability of oral insulin, such absorption enhancers, enzyme inhibitors, enteric coatings are also introduced. The potential absorption mechanisms of insulin-loaded nanoparticles across the intestinal epithelium, including intestinal lymphatic route, transcellular route and paracellular route are discussed in this review. Natural polymers, such as chitosan and its derivates, alginate derivatives, g-PGA-based materials and starch-based nanoparticles have been exploited for oral insulin delivery; synthetic polymers, such as PLGA, PLA, PCL and PEA have also been developed for oral administration of insulin. This review focuses on recent advances in using biodegradable natural and synthetic polymers for oral insulin delivery along with their future prospects.

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“…Semakin banyak terjadi reaksi sambung silang ionik antara kitosan dan STPP, maka semakin banyak molekul nanopartikel zat aktif yang terbentuk. Pada penelitian Yu-Hsin et al (2008) melaporkan bahwa STPP sebagai polianion berinteraksi membentuk ikatan silang dengan kitosan yang bersifat kation akan membentuk nanopartikel yang lebih stabil dan memiliki penembusan membran yang lebih baik. STPP dipilih memiliki sifat food grade, lebih aman, dan tidak menimbulkan efek samping.…”

Section: Sintesis Nanopartikel Kulit Manggisunclassified

Sintesis Nanopartikel Ekstrak Kulit Manggis Merah Dan Kajian Sifat Fungsional Produk Enkapsulasinya

Ningsih

Yasni

Yuliani

2017

jtip

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Utilization of mangosteen fruit waste tends to be less practical, so nanoparticle based encapsulation is an effective approach. The objective if this research was to utilize the waste from the red mangosteen peel Garcinia forbesii (GF) and Garcinia mangostana (GM ABSTRAKPemanfaatan limbah kulit buah manggis cenderung kurang praktis, sehingga enkapsulasi berbasis nanopartikel merupakan pendekatan yang efektif. Tujuan penelitian ini adalah pemanfaatan limbah kulit manggis merah Garcinia forbesii (GF) dan Garcinia mangostana (GM) untuk menghasilkan nanopartikel ekstrak, produk enkapsulasinya, dan mengetahui sifat fungsionalnya. Penelitian ini terdiri dari tiga tahap, yaitu ekstraksi, sintesis nanopartikel, dan enkpasulasi. Parameter yang digunakan adalah rendemen ekstrak, nilai fungsional antioksidan dan Total Senyawa Fenol (TSF), ukuran partikel, indeks polidispersitas, dan morfologi permukaan enkapsulat. Sintesis nanopartikel dilakukan menggunakan metode gelasi ionik. Perhitungan nilai fungsional menggunakan konsentrasi ekstrak sebesar 10% dalam larutan nanopartikel. Hasil penelitian menunjukkan bahwa menggunakan metode refluks memberikan hasil yang lebih baik dibandingkan dengan metode maserasi. Formula 2 nanopartikel dengan konsentrasi kitosan 0,2% dan STPP 0,1% dan produk enkapsulasinya dengan bahan penyalut Maltodekstrin Kasein (MK) memberikan hasil yang terbaik dengan peningkatan nilai fungsional.Kata kunci: enkapsulasi, kulit manggis merah, nanopartikel PENDAHULUAN1Salah satu buah Indonesia yang potensial berkhasiat bagi kesehatan adalah buah manggis. Walaupun kulit buah manggis tergolong dalam limbah, namun mengandung senyawa zat aktif yang berkhasiat bagi kesehatan. Buah manggis ada berbagai jenis, salah satunya manggis merah (Garcinia forbesii) atau dikenal dengan nama mundar dan

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Multi-ion-crosslinked nanoparticles with pH-responsive characteristics for oral delivery of protein drugs

Cited by 182 publications

References 38 publications

A novel ligand conjugated nanoparticles for oral insulin delivery

A novel ligand conjugated nanoparticles for oral insulin delivery

A review of biodegradable polymeric systems for oral insulin delivery

Sintesis Nanopartikel Ekstrak Kulit Manggis Merah Dan Kajian Sifat Fungsional Produk Enkapsulasinya

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