Matrix compositions for controlled release of peptide and polypeptide molecules
A matrix composition and molecular technology, applied in the direction of drug combination, peptide/protein composition, drug delivery, etc., can solve problems such as poisoning, horizontal oscillation, etc.
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[0216] The preparation process of the matrix according to the invention comprises only one step, in which an aqueous solution can be used. This solution is mixed with an organic volatile solvent, and all liquid is then removed. The process of the invention is thus able to achieve lipid saturation. Lipid saturation confers on the matrix composition the ability to resist substantial degradation in vivo; thus, the matrix composition exhibits the ability to mediate extended release on the scale of weeks or months.
[0217] In another embodiment, the matrix composition is dry. In another embodiment, "dry" refers to the absence of detectable amounts of water or organic solvents.
[0218] In another embodiment, the water permeability of the matrix composition has been minimized. "Minimizing" water permeability refers to the process of producing a matrix composition primarily in an organic solvent, as described herein, in the presence of lipids in an amount that has been determined...
Embodiment 1
[0226] Example 1 - Platform Technology Used to Generate Drug Carrier Compositions for Delivery of Peptide Molecules
[0227] I. Preparation of the first solution
[0228] Mix a polymer (e.g. PLGA, PGA, PLA or combinations thereof) and a sterol (e.g. cholesterol) and / or α-tocopherol or γ-tocopherol into a volatile organic solvent (e.g. with / without chloroform of ethyl acetate). The whole process is carried out at room temperature. Thus, a lipid-polymer matrix is obtained.
[0229] II. Preparation of the second solution
[0230] Dissolve at least one molecule selected from peptides, proteins, or any combination thereof in a volatile organic solvent (typically N-methylpyrrolidone, ethanol, methanol, ethyl acetate, or a combination thereof) or water and add polyethylene glycol (PEG ) 1,000-8000, usually PEG5,000. Phospholipids are added directly when the peptide molecules are dissolved in the organic solvent. When the peptide molecules are dissolved in water, the resulting...
Embodiment 2
[0246] Example 2: Preparation of matrices comprising antimicrobial peptides without PEG
[0247] The antimicrobial peptide used was Temporin-L (SEQ: FVQWFSKFLGRIL) labeled at its N-terminus with the fluorescent dye NBD.
[0248] 1. Peptide (1 mg) was dissolved in MeOH / EA and this solution was used in order to generate matrix formulation without PEG.
[0249] 2. Dissolve DPPC in the peptide solution to a final concentration of 225 mg / ml.
[0250] 3. PLGA75 / 25 was dissolved in ethyl acetate (300 mg / ml).
[0251] 4. Dissolve cholesterol in ethyl acetate (30 mg / ml).
[0252] 5. Mix one volume of PLGA solution with 5 volumes of cholesterol solution.
[0253]6. Mix two volumes of DPPC-peptide solution with three volumes of PLGA-cholesterol solution.
[0254] 7. Weigh 100 mg of tricalcium phosphate granules (TCP) into a 4 ml glass bottle.
[0255] 8. Add 0.15 ml of PLGA-cholesterol-DPPC peptide solution to the TCP particles. The resulting solution was incubated at 45°C until al...
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Abstract
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