Cholesterol-Based Microspheres for Macrocyclic Lactone Delivery
Find Innovative SolutionsGenerate Solutions
Solution Overview
Problem
Current sustained-release parenteral formulations of macrocyclic lactones, such as milbemycins and avermectins, face challenges due to their lipophilic nature, requiring oily or fatty bases, and often result in variable bioavailability and toxicity concerns, necessitating a more stable and safer delivery method.
Innovation Solution
Injectable microspheres containing 1-20% macrocyclic lactones, 50-95% fat or wax, 0.1-10% cholesterol, and 0.01-1% antioxidant, which provide sustained release and improved bioavailability, with cholesterol enhancing stability and tolerability, allowing for a single annual administration.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If oily or fatty bases are used to formulate macrocyclic lactones, then the lipophilic nature of the drug is accommodated, but variable bioavailability and toxicity concerns arise
Solution Approach 1:
The patent changes the physical-chemical parameters of the formulation by using cholesterol (a sterol) instead of conventional oily or fatty bases. This parameter change in the excipient type provides stable bioavailability while reducing toxicity, as cholesterol is a naturally occurring substance with established safety profiles in veterinary medicine.
Solution Approach 2:
The patent creates a composite microspherical formulation combining macrocyclic lactone active ingredients with cholesterol and other excipients. This composite material approach allows the formulation to accommodate the lipophilic nature of the drug while providing controlled release and reduced toxicity through the synergistic effects of the composite components.
2Duration of action of moving object
If conventional sustained-release formulations are used, then extended release is achieved, but uniform bioavailability across various animal species is not ensured
Solution Approach 1:
The patent achieves universality by formulating microspheres with cholesterol that can be applied across multiple animal species (dogs, cats, horses, cattle, sheep, goats, pigs). The cholesterol-based formulation provides consistent sustained-release characteristics and uniform bioavailability regardless of the species, making the formulation broadly applicable in veterinary medicine.
3Reliability
If frequent administrations are required to maintain therapeutic efficacy, then parasite coverage is improved, but therapeutic safety and animal well-being are compromised
Solution Approach 1:
The patent implements continuity of useful action through sustained-release microspheres that maintain therapeutic levels of macrocyclic lactones over an extended period (at least 6 months). This continuous release mechanism ensures consistent parasite coverage while reducing the frequency of administrations, thereby improving therapeutic safety and animal well-being by minimizing repeated injections and associated stress.
Applied Scientific Principles
This section explains which scientific principles are used to turn an abstract innovation direction into a practical engineering solution.
Function Achieved in This Case
The microspheres offer extended therapeutic efficacy for over 6 months, ensuring uniform bioavailability across various animal species, reduced toxicity, and effective prevention and treatment of endo- and ectoparasites with a single annual administration, enhancing animal health and safety.
Implementation Method 1
The microspheres according to the invention present the advantage, due to the presence of cholesterol, of stable release of moxidectin in the physiological temperature range of 36-40°C, thus guaranteeing uniform bioavailability characteristics in various animal species.
Implementation Method 2
The microspheres offer extended therapeutic efficacy for over 6 months, ensuring uniform bioavailability across various animal species
Data Source
Figure 1
Figure 2
Figure 3
AI summary
Disclosed are microspheres containing 1% to 20% by weight of milbemycin, avermectin or a derivative thereof, 50% to 95% by weight of a fat, a wax or a mixture thereof, 0.1 % to 10% by weight of a steroid lipid, preferably cholesterol, and 0.01% to 1% by weight of an antioxidant.