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Enteric-coated capsule containing cationic nanoparticles for oral insulin delivery

A nanoparticle and enteric coating technology, which is applied in capsule delivery, powder delivery, freeze-drying delivery, etc., can solve the problems of reducing the stability of nanoparticles and reducing the positive charge characteristics of nanoparticles

Active Publication Date: 2013-02-06
NANO & ADVANCED MATERIALS INST
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, mucoadhesive and pH-sensitive polycationic nanoparticles may be non-synergistic carriers of insulin because the positive charge of the polymer in these nanoparticles may reduce the stability of the nanoparticles in the stomach, and these The pH-sensitivity of polymers in nanoparticles may reduce the positive charge properties of nanoparticles in the intestine (Biomaterials 2009, 30:2329-2339)

Method used

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  • Enteric-coated capsule containing cationic nanoparticles for oral insulin delivery
  • Enteric-coated capsule containing cationic nanoparticles for oral insulin delivery
  • Enteric-coated capsule containing cationic nanoparticles for oral insulin delivery

Examples

Experimental program
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Effect test

Embodiment 1

[0027] Preparation of Cationic Nanoparticles Loaded with Insulin

[0028] Nanoparticles were prepared by multiple emulsification technique. Briefly, 1 mL of aqueous insulin solution (1 mg / mL) was first emulsified in dichloromethane (5 mL) containing 100 mg of polymer (PLGA / Eudragit RS, 50 / 50) by sonication at a power of 40 W for 30 s. The obtained first emulsion was then poured into 40 mL of polyvinyl alcohol aqueous solution (1%) and sonicated with a power of 60 W for 1 min, so that multiple emulsions were formed. After dichloromethane was evaporated under reduced pressure, nanoparticles were collected by centrifugation at 20,000 rpm for 10 minutes and washed three times. After pre-freezing the resulting dispersion overnight at -20°C (nanoparticle and cryoprotectant concentrations of 1% and 1.5%, respectively), the mixture was then vacuum lyophilized.

[0029] Table 1

[0030]

[0031]

[0032] Δ: Precipitation / aggregation of nanoparticles was observed.

[0033] The...

Embodiment 2

[0035] Characterization of insulin-loaded cationic nanoparticles

[0036] In general, nanoparticles have greater cellular uptake than microparticles and are more readily available for wider uptake due to their smaller size and greater fluidity. Reducing the nanoparticle size results in increased absorption of insulin by enterocytes. Many formulation and process parameters affecting nanoparticle size, such as sonication time, polymer amount, surfactant concentration, and volume of oil phase and external aqueous phase, etc., were investigated in the multiple emulsion solvent evaporation method in the present invention. Changing the volume of the external aqueous phase is considered to be the easiest way to adjust the size of the nanoparticles of the invention. As shown in Table 2, reducing the volume of the external aqueous phase can reduce the size of the nanoparticles and increase the zeta potential value of the nanoparticles. The smaller the volume of the outer aqueous phas...

Embodiment 3

[0041] Zeta potential of PLGA / RS nanoparticles under different pH conditions

[0042] The zeta potential value is an important particle property as it can affect both nanoparticle stability and mucoadhesion under GI conditions. Positive zeta potential values ​​can promote mucoadhesion. The mucosal layer itself is at neutral pH with anionic polyelectrolytes. Therefore, the presence of positively charged groups on the nanoparticles can induce charge interactions between the mucosa and the particles. As shown in Table 3, the zeta potential values ​​and sizes of PLGA / RS nanoparticles have been investigated in the pH range of 1.2-7.2, which mimics GI physiological conditions. Obviously the pH value of the medium has an important effect on the zeta potential value of the nanoparticles. In general, quaternary ammonium cations in RS polymers are permanently charged independent of the pH of their solutions. Insulin (PI=5.4) becomes a positively charged molecule at pH 1.2. Theoreti...

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Abstract

The invention relates to an enteric-coated capsule containing cationic nanoparticles for oral insulin delivery, in particular to a type of cationic nanoparticle including a polycationic and mucoadhesive polymer and a biodegradable polymer, wherein each of the nanoparticles has positive surface charge and enhanced permeability for paracellular insulin delivery; the enteric-coated capsule further includes a pH-sensitive polymer as the coating. The enteric-coated capsule containing cationic nanoparticles, when being orally administered to a subject, are configured to prevent the acidic degradation of the active substance such as insulin before being released from said cationic nanoparticles to a specific absorption site along the gastrointestinal tract.

Description

[0001] Cross References to Related Applications [0002] This application claims priority to US Provisional Application Serial No. 61 / 573,014, filed August 4, 2011, the disclosure of which is incorporated herein by reference. technical field [0003] The present invention relates to enteric-coated capsules comprising cationic nanoparticles for oral insulin delivery, and more particularly, to enteric-coated capsules comprising cationic nanoparticles loaded with insulin, each nanometer The particles contain a class of polycationic polymers capable of controlling the release of insulin. The invention also relates to a process for the preparation of cationic nanoparticles and enteric-coated capsules comprising said cationic nanoparticles. Background technique [0004] Multiple daily insulin injections remain the traditional approach for treating insulin-dependent diabetics (Drug Discovery Today 2001, 6: 1056-1061). However, disadvantages associated with this therapy are subopt...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/48A61K9/19A61K47/34A61K47/38A61K47/32A61K47/36A61K38/28A61P5/48
Inventor 钱宇章莉娟吴志民周丽英蒋薇凌莉罗茜郭新东
Owner NANO & ADVANCED MATERIALS INST
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