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Publication Number
US-12138346-B2
Publication Date
2024-11-12
Expiration Date
Abstract
A bioactive substance delivery system includes a bioactive substance comprising nucleic acid, and a bioactive substance carrier comprising a porous silica particle having a plurality of pores with a diameter of 5 nm to 100 nm, and having not less than 24 hours at which a ratio of absorbance is ½. The porous silica particles may be positively charged inside the pore at neutral pH.
Core Innovation
A bioactive substance delivery system is provided that includes a bioactive substance comprising nucleic acid and a bioactive substance carrier comprising a porous silica particle. The porous silica particle has a plurality of pores with a diameter of 5 nm to 100 nm and includes a degradability criterion characterized by a time t of not less than 24 hours.
The degradability criterion is defined by an absorbance ratio measured by Equation 1, where A0 denotes an absorbance of the porous silica particle measured after placing the particle suspension in a cylindrical permeable membrane and measuring after setting conditions with pH 7.4. At time t, At is the absorbance of the porous silica particles measured t hour after the measurement of A0, and the ratio At/A0 is 1/2.
The porous silica particles are described as positively charged inside the pore at neutral pH. The porous silica system further supports delivery of nucleic acids and is associated with biodegradability and sustained release behavior over hours to days, with tunable degradation using properties such as surface substituents/charge and particle parameters including pore size, particle size, BET surface area, and pore volume.
Claims Coverage
The independent claim (1) defines a bioactive substance delivery system with nucleic acid and a porous silica particle characterized by pore diameter (5 nm to 100 nm), a specified durability criterion based on an absorbance ratio (At/A0=1/2) with t≥24 hours as defined by Equation 1, and a positive charge inside the pore at neutral pH. Inventive features concentrate on four elements.
Nucleic acid bioactive substance for delivery
A bioactive substance delivery system comprising a bioactive substance comprising nucleic acid.
Porous silica carrier with 5–100 nm pores
A bioactive substance carrier comprising a porous silica particle having a plurality of pores with a diameter of 5 nm to 100 nm.
Durability criterion defined by absorbance ratio with t≥24 hours
The porous silica particle has t of not less than 24 hours, at which a ratio of absorbance measured by Equation 1 is 1/2, where A0 and At are absorbances defined by the measurement scheme of Equation 1.
Positive charge inside pore at neutral pH
The porous silica particles is positively charged inside the pore at neutral pH.
Across the provided independent-claim material, the inventive coverage centers on combining a nucleic-acid bioactive substance with a porous silica carrier having 5–100 nm pores, enforcing a specific absorbance-ratio degradability/durability metric (At/A0=1/2 at t≥24 hours) as defined by Equation 1, and requiring the porous silica to be positively charged inside the pore at neutral pH.
Stated Advantages
Provides biodegradability and sustained release behavior over hours to days.
Documented Applications
In vitro mouse siRNA delivery is described, including observations of siRNA release.
In vitro intracellular delivery observations are described for Cas9, together with intracellular delivery context using labels/fluorescence imaging elements (e.g., FOBI fluorescence imaging; FITC/FAM/Cy5 labels).
Tumor-related demonstration is described using HeLa xenograft tumors.
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