COMPOSITION AND METHOD FOR THE DELIVERY OF BIOLOGICS USING NANOPARTICLES

Abstract

COMPOSITION AND METHOD FOR THE DELIVERY OF BIOLOGICS USING NANOPARTICLES ABSTRACT This invention relates to a composition and method for delivering biologics using nanoparticles. The system encapsulates biologic agents within biodegradable nanoparticles, enhancing stability and targeted delivery. The nanoparticles are prepared from biocompatible polymers, such as PLGA, using an emulsification method. Upon administration, the nanoparticles release the biologic in a controlled manner, optimizing therapeutic efficacy while reducing systemic side effects. This invention offers a significant improvement in the bioavailability of biologics, including proteins and nucleic acids, for therapeutic applications.

Specification

Description:COMPOSITION AND METHOD FOR THE DELIVERY OF BIOLOGICS USING NANOPARTICLES

FIELD OF THE INVENTION

The present invention relates to the field of biotechnology and pharmaceutical sciences. More specifically, it pertains to a composition and method for the efficient delivery of biologic agents, such as proteins, peptides, nucleic acids, and vaccines, using nanoparticles as carriers. The invention addresses challenges in targeted delivery, stability, and bioavailability of biologics in therapeutic applications.

BACKGROUND OF THE INVENTION

Biologic agents, including therapeutic proteins, peptides, and nucleic acids, are crucial in modern medicine due to their high specificity in treating various diseases, including cancers, autoimmune disorders, and genetic conditions. However, despite their therapeutic potential, biologics face significant delivery challenges that hinder their widespread use. These challenges include poor bioavailability, rapid degradation by proteases and nucleases, immune system activation, and difficulty in targeting specific cells or tissues.
Traditional drug delivery methods often fail to protect biologics from premature degradation, leading to reduced therapeutic efficacy and increased systemic side effects. Moreover, the high molecular weight and hydrophilicity of biologics limit their ability to penetrate biological membranes, making targeted and controlled release delivery essential for achieving desired therapeutic outcomes.
Nanoparticle-based delivery systems have emerged as a promising approach for improving the stability and bioavailability of biologics. Nanoparticles can encapsulate biologic agents, shielding them from degradation, facilitating targeted delivery to specific tissues, and enabling sustained release. Despite these advancements, the optimization of nanoparticle formulations for biologic delivery remains a complex task, with challenges including low drug-loading capacity, non-specific interactions, and lack of precise control over release profiles.
The present invention aims to overcome these limitations by providing a novel nanoparticle-based delivery system designed specifically for biologics. The invention addresses critical challenges in biologic delivery, such as protecting biologics from degradation, enhancing cellular uptake, and ensuring sustained and controlled release of the therapeutic agent.

SUMMARY OF THE INVENTION

In an embodiment, the present invention provides a composition and method for the delivery of biologics using nanoparticles as carriers. The nanoparticle-based delivery system is designed to protect biologics from degradation, improve their bioavailability, and facilitate targeted delivery to specific tissues or cells.
The invention includes a biodegradable nanoparticle composition, wherein the biologic agent is encapsulated within a polymer matrix made from biocompatible materials such as poly(lactic-co-glycolic acid) (PLGA), chitosan, or other suitable polymers. The nanoparticles are prepared using methods such as emulsification, solvent evaporation, or nanoprecipitation, allowing for efficient encapsulation of the biologic.
The method for delivery involves administering the nanoparticle composition to a subject, wherein the nanoparticles release the biologic in a controlled manner at the target site. The system is designed to offer sustained release of the biologic, enhancing therapeutic efficacy while minimizing systemic exposure and side effects. The targeting capabilities of the nanoparticles can be further enhanced by incorporating ligands on their surface, facilitating site-specific delivery.
In summary, the invention offers a significant improvement over traditional biologic delivery systems by providing enhanced stability, controlled release, and targeted delivery of biologic agents, leading to improved therapeutic outcomes.


BRIEF DESCRIPTION OF THE FIGURES

The accompanying figure illustrates the method for preparing and administering the nanoparticle-based biologic delivery system. The figure includes:
1. Nanoparticle synthesis using a polymer matrix.
2. Encapsulation of the biologic within the nanoparticle.
3. Administration of the composition to the subject.
4. Targeted release of the biologic at the site of action.

DETAILED DESCRIPTION OF THE INVENTION

The invention relates to a novel nanoparticle-based system for the delivery of biologics. In an embodiment, the system consists of nanoparticles that encapsulate biologic agents such as proteins, peptides, and nucleic acids, protecting them from degradation and enhancing their bioavailability. The nanoparticles are formed from biodegradable, biocompatible polymers, including poly(lactic-co-glycolic acid) (PLGA), chitosan, or polycaprolactone (PCL).
Nanoparticle Synthesis
The nanoparticles are synthesized using a solvent evaporation technique. In an embodiment, PLGA is dissolved in an organic solvent such as dichloromethane (DCM) or ethyl acetate. The biologic agent is dissolved in an aqueous phase, which is emulsified with the polymer solution to form a water-in-oil (W/O) emulsion. This emulsion is subjected to high-speed homogenization to achieve nanoparticle size. Subsequently, the solvent is evaporated under reduced pressure, allowing the polymer to solidify, forming nanoparticles that encapsulate the biologic.
The size and morphology of the nanoparticles can be controlled by adjusting parameters such as polymer concentration, emulsification speed, and solvent evaporation rate. Nanoparticles typically range from 50 to 200 nanometers in diameter, ensuring efficient cellular uptake and minimizing clearance by the reticuloendothelial system (RES).
Biologic Encapsulation and Stability
The encapsulation efficiency of the biologic agent depends on factors such as the physicochemical properties of the biologic, the polymer composition, and the preparation method. In an embodiment, the invention ensures high encapsulation efficiency by optimizing the polymer-to-biologic ratio during nanoparticle synthesis. The biologic is encapsulated within the nanoparticle core, shielding it from enzymatic degradation and maintaining its activity during circulation.
To enhance stability, the nanoparticles can be lyophilized (freeze-dried) and reconstituted before administration. Cryoprotectants, such as trehalose or mannitol, may be added to the formulation to prevent aggregation during lyophilization.
Targeted Delivery and Controlled Release
The nanoparticles are designed to release the biologic in a controlled manner at the target site. The rate of release can be tailored by modifying the polymer composition or incorporating additives that alter the degradation rate of the polymer matrix. For example, increasing the lactic acid content in PLGA will slow down the degradation rate, resulting in sustained release over a longer period.
In an embodiment, the nanoparticles are coated with targeting ligands such as antibodies or peptides, which bind to specific receptors on the surface of target cells. This targeting capability ensures that the biologic is delivered directly to the site of action, reducing systemic side effects and improving therapeutic outcomes.
Administration
The nanoparticle composition can be administered via various routes, including intravenous injection, subcutaneous injection, or oral administration. In an embodiment, the nanoparticles are suspended in an isotonic buffer solution for intravenous injection. The nanoparticles can also be incorporated into a solid dosage form, such as capsules or tablets, for oral delivery.
Upon administration, the nanoparticles circulate in the bloodstream and accumulate at the target site, where the biologic is released. The release profile is controlled by the degradation rate of the polymer and the diffusion of the biologic from the nanoparticle core. In some embodiments, external stimuli such as pH or temperature may be used to trigger the release of the biologic from the nanoparticles.
Enhanced Stability of Biologics: The nanoparticle system encapsulates biologics, protecting them from enzymatic degradation and environmental factors, significantly improving their stability during storage and in vivo.

Improved Bioavailability: By encapsulating biologics in nanoparticles, the system enhances the bioavailability of therapeutic agents, allowing more efficient delivery to target tissues or cells.
Controlled Release: The biodegradable nature of the nanoparticles allows for sustained and controlled release of biologics, reducing the need for frequent dosing and improving therapeutic efficacy.
Targeted Delivery: Surface modifications, such as ligand conjugation, enable the nanoparticles to target specific cells or tissues, minimizing off-target effects and maximizing therapeutic impact at the desired site.
Reduced Side Effects: Targeted delivery and controlled release reduce systemic exposure to biologics, minimizing potential side effects and enhancing patient safety.
Versatile Encapsulation: The system is adaptable to a wide range of biologics, including proteins, peptides, nucleic acids, and vaccines, making it versatile for various therapeutic applications.
Biocompatibility and Biodegradability: The nanoparticles are made from biocompatible and biodegradable polymers, ensuring safe metabolism and clearance from the body without causing toxic effects.
Enhanced Cellular Uptake: Nanoparticles, due to their small size, can efficiently penetrate cellular membranes, enhancing the uptake of biologics by target cells and increasing therapeutic efficiency.
Customizable Release Profiles: By altering the composition of the polymer matrix, the degradation rate and release profile of the biologic can be tailored, allowing for precise control over drug delivery timing.
Reduced Immune Activation: The encapsulation of biologics within nanoparticles helps to shield them from immediate recognition by the immune system, reducing the likelihood of immune responses that could limit their therapeutic effect.
, C , Claims:I/WE CLAIM:
Claim 1
A method for delivering biologic agents using nanoparticles, comprising:
• a) preparing a biodegradable nanoparticle composition by encapsulating a biologic agent within a biocompatible polymer matrix;
• b) administering the nanoparticle composition to a subject; and
• c) releasing the biologic agent in a controlled manner at a target site within the subject.
Claim 2
The method of claim 1, wherein the biocompatible polymer is poly(lactic-co-glycolic acid) (PLGA).
Claim 3
The method of claim 1, wherein the biologic agent is a protein, peptide, or nucleic acid.
Claim 4
The method of claim 1, wherein the nanoparticles are prepared using an emulsification and solvent evaporation technique.
Claim 5
The method of claim 1, further comprising coating the nanoparticles with targeting ligands for site-specific delivery.
Claim 6
The method of claim 1, wherein the nanoparticle composition is suspended in an aqueous delivery medium prior to administration.
Claim 7
The method of claim 1, wherein the controlled release of the biologic agent is achieved by modifying the polymer degradation rate.
Claim 8
The method of claim 1, wherein the nanoparticle composition is administered via intravenous injection.
Claim 9
The method of claim 1, wherein the nanoparticle composition enhances the bioavailability of the biologic agent compared to non-encapsulated delivery.

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