Biodegradable Sustained Release Drug Formulations
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Solution Overview
Problem
Current drug delivery methods often result in high and low blood concentrations and short half-lives, requiring large doses that can lead to toxic side effects, and there is a need for more economical and efficient systems for sustained release of medications, especially for local or systemic treatments.
Innovation Solution
Development of biocompatible and biodegradable syringeable liquid, implantable solid, and injectable gel formulations using excipients like tocopherol isomers, benzyl benzoate, and polycarbonate oligomers for controlled and sustained release of active agents, allowing for extended release periods from a few days to several months.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If conventional drug delivery methods (topical, oral, intramuscular, intravenous, subcutaneous injection) are used, then drugs can be administered easily, but they result in high and low blood concentrations, short half-life, and may require large doses that cause toxic side effects
Solution Approach 1:
The patent prepares drug formulations in advance with controlled release characteristics, embedding the drug in a biodegradable matrix that will release the drug at a controlled rate over time. This preliminary preparation ensures that when administered, the drug delivers therapeutic levels consistently without requiring large initial doses that would cause toxicity.
Solution Approach 2:
The patent creates sustained-release formulations that continuously deliver therapeutic levels of drug over an extended period (days to months). This continuous action maintains stable blood concentrations, eliminating the peaks and troughs associated with conventional dosing, thereby providing reliable therapeutic efficacy without toxic side effects from overdosing.
2Ease of operation
If conventional drug delivery methods are used, then administration is simple, but the half-life in blood is shortened requiring frequent dosing
Solution Approach 1:
The patent employs biodegradable matrices that continuously release drug over extended periods (days to months), transforming short half-life drugs into long-acting formulations. This continuous release mechanism maintains therapeutic levels without requiring frequent re-administration, effectively extending the duration of action while keeping administration simple.
Solution Approach 2:
The patent changes the release rate parameter of the drug by controlling the degradation rate of the biodegradable matrix. By adjusting matrix composition and structure, the drug release kinetics are modified to match the desired half-life extension, allowing simple administration with prolonged duration of action.
3Reliability
If large doses are used to achieve therapeutic efficacy with conventional methods, then therapeutic effect is improved, but toxic side effects increase
Solution Approach 1:
The patent changes the concentration parameter over time by using controlled-release matrices. Instead of administering large initial doses, the formulation releases drug at controlled low rates that maintain therapeutic concentrations without exceeding toxic thresholds. This parameter transformation from high initial concentration to sustained low concentration eliminates toxicity while preserving efficacy.
Solution Approach 2:
The patent replaces bolus dosing with continuous low-level drug delivery. This continuous action maintains drug concentrations within the therapeutic window throughout the dosing interval, eliminating the high peaks that cause toxicity while ensuring adequate levels for efficacy are maintained continuously.
4Duration of action of moving object
If reservoir delivery systems (Vitrasert, Duros, Implanon) are used for sustained release, then drug delivery is extended, but the systems are complex and require surgical implantation
Solution Approach 1:
The patent changes the physical state parameter of the formulation, creating injectable forms that transform from liquid to gel or solid in situ. This eliminates the need for complex surgical implantation devices while achieving extended release periods, as the injected formulation self-assembles into a sustained-release depot at the injection site.
Solution Approach 2:
The patent employs formulations that self-form into sustained-release depots after injection. The biodegradable matrix self-assembles and maintains the drug reservoir function without requiring external mechanical structures or surgical implantation, allowing the system to serve itself by converting from injectable form to functional depot automatically.
5Duration of action of moving object
If biodegradable implants (Lupron Depot, Posurdex) are used, then sustained release is achieved, but manufacturing and production are complex
Solution Approach 1:
The patent employs liquid or semi-solid formulations that can be delivered through injection (hydraulic principle), eliminating complex manufacturing processes required for solid implant fabrication. The liquid formulation is easily manufactured, packaged, and sterilized using standard pharmaceutical techniques, then transforms into a sustained-release depot in vivo.
Solution Approach 2:
The patent changes the formulation from solid implant to liquid/injectable form, dramatically simplifying manufacturing. The liquid formulation can be prepared using standard mixing and filling processes, whereas solid implants require molding, sterilization, and assembly operations. The parameter change from solid to liquid state eliminates manufacturing complexity while maintaining sustained release functionality.
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
These formulations provide therapeutic levels of active agents over an extended period, primarily at the site of implantation, are non-toxic, and disappear harmlessly after use, offering a more efficient and economical solution for drug delivery compared to existing methods.
Implementation Method 1
the formulation exhibits an in vitro dissolution profile wherein about 2% to about 100% of the active agent is released over a period ranging from about 1 day to at least 365 days
Implementation Method 2
sustained release of an active agent comprising a biocompatible, biodegradable excipient and an active agent
Implementation Method 3
The formulations are both biocompatible and biodegradable, and disappear harmlessly after delivering active agent to the desired site
Data Source
AI summary
This invention provides for biocompatible and biodegradable syringeable liquid, implantable solid, and injectable gel pharmaceutical formulations useful for the treatment of systemic and local disease states.