Dose, localization, and formulation of botulinum toxins in skin and muscle

摘要

Formulations of and dosing protocols for the administration of botulinum toxin that maximize efficacy and specificity while minimizing the likelihood of overdosing and undesirable side effects of treatment. The formulations include positively charged carriers, such as cationic peptides, which otherwise have no inherent botulinum-toxin-like activity. The dosing regimen is based on the pattern, quantity, and location of neuromuscular junctions in the target tissue. Because the number of neuromuscular junctions in a target tissue remains generally stable throughout life and because the pharmacological effect of botulinum toxin is localized at the neuromuscular junction, dosing efficacy is unaffected by muscle mass, age of the patient, or body weight.

主权项

1. A method for dosing botulinum toxin in a human target muscle to effect a desired treatment while limiting toxin diffusion to non-targeted tissues comprising the steps of:
a) determining the mass of a target muscle; b) determining the distribution pattern and location of neuromuscular junctions (NMJ) in said target muscle; and, c) delivering doses of a botulinum toxin A formulation with a charged backbone by intramuscular injection around said distribution pattern and location of said target muscle neuromuscular junctions within a range of about 0.1 cm to about 3.0 cm of said target muscle neuromuscular junctions distribution pattern in an amount corresponding to the quantity of said neuromuscular junctions in said target muscle and the mass of said target muscle.