Enteric-coated capsules filled with freeze-dried chitosan/poly(γ-glutamic acid) nanoparticles for oral insulin delivery

Sonaje, Kiran; Chen, Yijia; Chen, Hsin‐Lung; Wey, Shiaw-Pyng; Juang, Jyuhn‐Huarng; Nguyen, Ho-Ngoc; Hsu, Chia‐Wei; Lin, Kun-Ju; Sung, Hsing‐Wen

doi:10.1016/j.biomaterials.2010.01.042

Cited by 270 publications

(175 citation statements)

References 36 publications

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“…As for all lecithin/chitosan NPs (A2, A3, C2 and C3 samples), no considerable difference in the mean particle size, size distribution, zeta potential or melatonin content before and after freeze-drying and reconstitution were observed. Similar observations were already reported in the literature: comparable mean particle diameters, polydispersities and zeta potentials before and after freeze-drying have been reported for positively charged chitosan/poly(g-glutamic acid) nanoparticles lyophilised in the presence of 1.5 or 2.5% trehalose 20) and for chitosan/TPP nanoparticles lyophilised in the presence of 2.5 or 5% glucose. 19) However, a deviation higher than 10% in the mean NP diameter before and after freeze-drying was observed for the chitosan-free lecithin NPs (samples A1 and C1; Fig.…”

Section: Resultssupporting

confidence: 91%

Short- and Long-Term Stability of Lyophilised Melatonin-Loaded Lecithin/Chitosan Nanoparticles

Hafner

Dürrigl

Pepić

et al. 2011

CHEMICAL & PHARMACEUTICAL BULLETIN

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Regular ArticleRecently, attention has been paid to lecithin/chitosan nanoparticles (NPs) as an alternative colloidal carrier system to polymeric nanoparticles, solid lipid nanoparticles, liposomes and nanoemulsions. These nanoparticles were obtained from the supra-molecular self-organising interaction of the negatively charged lipid material lecithin and the positively charged polysaccharide chitosan, without preliminary vesicle formation.1,2) These constitutive materials are favoured due to their well-known characteristics: Chitosan is a biocompatible and biodegradable cationic polysaccharide exhibiting bioadhesive and penetration enhancing properties 3) ; lecithin is a natural lipid mixture of phospholipids, mainly phosphatidylcholine and phosphatidylethanolamine, and is considered a safe and biocompatible excipient that has been frequently used for the preparation of various delivery nanosystems, such as micro-and nanoemulsions, 4) liposomes, 5) micelles 6) and solid lipid nanoparticles. 7)Mucoadhesive lecithin/chitosan NPs were shown to be suitable carriers for lipophilic drugs. NP suspension prepared with Lipoid S45 lecithin with a lecithin-to-chitosan weight ratio of 20 : 1 enhanced melatonin permeability through a Caco-2 cell monolayer compared to its permeability in an aqueous solution, without inducing plasma membrane damage or a decrease in cell viability at the concentration tested. 8) In another study, lecithin/chitosan NP dispersion was shown to increase accumulation of clobetasol-17-propionate in the skin without any significant permeation across the skin, compared to chitosan gel and commercial cream. 9)These findings imply that lecithin/chitosan NPs have great potential to improve the permeation of encapsulated drugs across various biological barriers. However, the overall poor stability of colloidal nanoparticles in an aqueous medium is a significant drawback from a development perspective. Thus, one of the most important challenges in the development of nanoparticles is to achieve long-term stability during storage.Freeze-drying is a well-established approach to increase the chemical and physical stability of colloidal systems over extended time periods. Prior to the freeze-drying process, special excipients are usually added to the formulation to protect the nanoparticles from various stresses generated during the freezing and drying steps. The role of sugars, such as sorbitol, mannitol, trehalose, glucose, sucrose, and lactose, as lyoprotective and/or cryoprotective agents to prevent nanoparticle aggregation and improve the redispersibility of the dry product has been reviewed in the literature. 10) Briefly, stabilisation of materials in sugar glasses has been explained by the formation of a glassy sugar matrix, which acts as a physical barrier between the particles 11) and inhibits diffusion on a relevant time scale. 12) Recently, Zhang et al. reported that sugars such as glucose and trehalose are very effective in preventing particle aggregation and inhibiting leakage of an active ingredie...

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Section: Resultssupporting

confidence: 91%

Short- and Long-Term Stability of Lyophilised Melatonin-Loaded Lecithin/Chitosan Nanoparticles

Hafner

Dürrigl

Pepić

et al. 2011

CHEMICAL & PHARMACEUTICAL BULLETIN

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“…In addition, the major drawback of the formulation was that the NPs became unstable and disintegrated in the alkaline pH of the gastrointestinal tract, limiting its potential for the oral delivery of insulin. Hence, to overcome the issue, the same group freeze-dried the NPs and delivered it orally through an enteric-coated capsule (93). Small angle X-ray scattering profiles of insulin showed that the structure of insulin remained same in spite of going through the process of freeze drying and it neither got fragmented nor aggregated upon release.…”

Section: Chitosan and Its Derivatives Combined With Different Peptidesmentioning

confidence: 99%

Recent Advancement of Chitosan-Based Nanoparticles for Oral Controlled Delivery of Insulin and Other Therapeutic Agents

2010

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Abstract. Nanoparticles composed of naturally occurring biodegradable polymers have emerged as potential carriers of various therapeutic agents for controlled drug delivery through the oral route. Chitosan, a cationic polysaccharide, is one of such biodegradable polymers, which has been extensively exploited for the preparation of nanoparticles for oral controlled delivery of several therapeutic agents. In recent years, the area of focus has shifted from chitosan to chitosan derivatized polymers for the preparation of oral nanoparticles due to its vastly improved properties, such as better drug retention capability, improved permeation, enhanced mucoadhesion and sustained release of therapeutic agents. Chitosan derivatized polymers are primarily the quaternized chitosan derivatives, chitosan cyclodextrin complexes, thiolated chitosan, pegylated chitosan and chitosan combined with other peptides. The current review focuses on the recent advancements in the field of oral controlled release via chitosan nanoparticles and discusses about its in vitro and in vivo implications.

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“…Similar results were rendered using chitosan nanocarriers designed for pH-sensitive release and enhanced mucoadhesive potential, resulting in improved absorption of anti-diabetic drugs (Wong, 2010). A combination of classical oral delivery formulations and nanotechnologies, e.g., chitosan nanocarriers encased within enteric-coated capsules for insulin delivery, has shown enhanced results, reflecting the potential of nanomedicine to impact oral delivery of active therapeutics (Cui, et al, 2009, Sonaje, et al, 2010.…”

Section: Small Molecule Therapymentioning

confidence: 78%

Nanomedicine and Drug Delivery Strategies for Treatment of Genetic Diseases

Hsu¹,

Muro²

2011

Human Genetic Diseases

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Enteric-coated capsules filled with freeze-dried chitosan/poly(γ-glutamic acid) nanoparticles for oral insulin delivery

Cited by 270 publications

References 36 publications

Short- and Long-Term Stability of Lyophilised Melatonin-Loaded Lecithin/Chitosan Nanoparticles

Short- and Long-Term Stability of Lyophilised Melatonin-Loaded Lecithin/Chitosan Nanoparticles

Recent Advancement of Chitosan-Based Nanoparticles for Oral Controlled Delivery of Insulin and Other Therapeutic Agents

Nanomedicine and Drug Delivery Strategies for Treatment of Genetic Diseases

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