Colloidal suspension of submicronic particles for carrying hydrophilic active principles (insulin) and method for preparing same
First Claim
1. Colloidal suspension of submicron particles capable of being used especially for carrying one or more active principles (AP), these particles being individualized supramolecular arrangements that are:
- based on an amphiphilic copolymer comprising;
at least one block of hydrophobic linear polyamino acid(s) (PAA) having α
-peptide linkages, the hydrophobic amino acids, AAO, constituting this PAA block being identical to or different from one another;
and at least one block of hydrophilic polymer(s) of the polyalkylene glycol (PAG) type, preferably of the polyethylene glycol (PEG) type;
and capable of associating with at least one AP in colloidal suspension, in the undissolved state, and releasing it, especially in vivo, in a prolonged and/or delayed manner, characterized in that the particles it contains are associated and/or can be associated with at least one AP selected from hydrophilic AP, preferably proteins, this AP consisting particularly preferably of insulin.
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Abstract
The invention concerns a suspension of particles for carrying hydrophilic active principles (insulin). Said carrier particles are based on a polyethylene glycol/hydrophobic neutral polyminoacid double-block polymer. Said polyethylene glycol/hydrophobic neutral polyaminoacid particles are associated with a hydrophilic active principle (insulin). The invention also concerns, a powdery solid from which the transporting particles are derived and the preparation of said solid and said suspension of transporting particles based on polyethylene glycol/hydrophobic neutral polyminoacid particles and insulin. Said preparation consists in copolymerising N-carboxy-anhydrides of hydrophobic neutral polyminoacid particles, in the presence of N-methyl/pyrrolidone, methanol, and amine-functionalised polyethylene glycol, thereby obtaining polyethylene glycol/hydrophobic neutral polyaminoacids, associating the latter with insulin; precipitating with water so as to obtain the carrier particles; optionally carrying out neutralisation, dialysis, concentration and elimination of water, thereby producing a powdery solid or suspended carrier particles and preparing pharmaceutical specialties.
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Citations
21 Claims
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1. Colloidal suspension of submicron particles capable of being used especially for carrying one or more active principles (AP), these particles being individualized supramolecular arrangements that are:
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based on an amphiphilic copolymer comprising;
at least one block of hydrophobic linear polyamino acid(s) (PAA) having α
-peptide linkages, the hydrophobic amino acids, AAO, constituting this PAA block being identical to or different from one another;
and at least one block of hydrophilic polymer(s) of the polyalkylene glycol (PAG) type, preferably of the polyethylene glycol (PEG) type;
and capable of associating with at least one AP in colloidal suspension, in the undissolved state, and releasing it, especially in vivo, in a prolonged and/or delayed manner, characterized in that the particles it contains are associated and/or can be associated with at least one AP selected from hydrophilic AP, preferably proteins, this AP consisting particularly preferably of insulin. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21)
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Specification