Berbamine Solid Lipid Nanoparticles via Aqueous Homogenization
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Solution Overview
Problem
Current methods for preparing berbamine nanoparticles are complex, involve organic solvents, and do not provide controlled release or high bioavailability, making them unsuitable for industrial viability and clinical use.
Innovation Solution
A process involving hot high-pressure homogenization to create solid lipid nanoparticles (SLNs) of berbamine, using GRAS components, which allows for high drug loading and controlled release without organic solvents, enhancing bioavailability and stability.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If conventional nanoparticle preparation methods are used, then nanoparticles can be formed, but the process becomes complex and involves organic solvents
Solution Approach 1:
The patent extracts and eliminates organic solvents from the nanoparticle preparation process by using solely aqueous phases. The method achieves nanoparticle formation through water-based surfactant systems, completely removing the need for organic solvents like ethanol or acetone that are typically required in conventional emulsification methods.
Solution Approach 2:
The patent segments the preparation process into distinct aqueous phases: a lipid-containing aqueous phase and a surfactant-containing aqueous phase. This segmentation allows each phase to perform its specific function while maintaining overall process simplicity and avoiding complex multi-step procedures involving organic solvents.
2Reliability
If conventional nanoparticle preparation methods are used, then nanoparticles can be formed, but toxicity increases due to organic solvent use
Solution Approach 1:
The patent converts the potential harm of requiring solvents for nanoparticle formation into a benefit by demonstrating that aqueous solvents alone are sufficient. This transforms the harmful organic solvent requirement into a beneficial water-based system that is non-toxic and biocompatible, while still achieving effective nanoparticle formation.
3Ease of manufacture
If simple preparation methods are used, then the process is easier to manufacture, but controlled release and high bioavailability are not achieved
Solution Approach 1:
The patent achieves controlled release through parameter changes in the aqueous phases, specifically by adjusting lipid concentration, surfactant concentration, pH, and temperature. These parameter modifications enable the simple aqueous-based process to produce nanoparticles with controlled release properties and high bioavailability, matching the performance of complex methods.
4Quantity of substance
If organic solvents are used in nanoparticle preparation, then the process can proceed, but industrial viability decreases
Solution Approach 1:
The patent extracts organic solvents from the industrial process, leaving only aqueous components. This extraction eliminates the need for costly solvent recovery systems, reduces safety requirements for handling flammable materials, and simplifies regulatory approval, thereby significantly improving industrial viability while maintaining process feasibility.
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 process results in berbamine SLNs with high drug loading, improved bioavailability, and controlled release, suitable for various delivery methods, including topical and dermatological applications, effectively addressing the limitations of previous methods.
Implementation Method 1
preparing a lipid phase by melting one or more lipid selected from the group consisting of glycerides and fatty acids at a temperature at least equal to the melting point of said one or more lipid
Implementation Method 2
adding the berbamine containing hot lipid phase of step (iii) to the aqueous phase of step (ii) or adding the berbamine containing aqueous phase of step (iii) to the lipid phase of step (i) and mixing at high speed of 5,000-20,000 rpm at the said pH for 5-30 min to obtain a primary coarse emulsion
Implementation Method 3
subjecting the primary coarse emulsion of step (iv) to two to six cycles of homogenization at 500 to 1200 bars to obtain solid lipid nanoparticles of berbamine
Data Source
AI summary
The present invention relates to a simple and convenient process for preparing solid lipid sustained release nanoparticles for berbamine delivery. The process involves preparation of nanoparticles by maintaining the pH of the aqueous or lipid phase so that high drug loading of 12-50% w/w with respect to the lipid matrix and high entrapment efficiency of more than 90% for berbamine in the solid lipid nanoparticles is achieved. The nanoformulation obtained by the process of the present invention has increased efficacy and exhibited any therapeutic property identical to free berbamine such as antiviral-cum-antibacterial agent for the treatment of microbial infections especially resistant Acinetobacter infections in treating diabetes and more specifically diabetes associated complications. Use may be extended to other diseases like COVID 19.