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Oral Nucleic Acid Formulation Development

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At CD Formulation, we are committed to leading the pioneering efforts in developing transformative oral nucleic acid solutions. Our team of skilled R&D specialists works diligently with state-of-the-art technology to significantly enhance the stability and absorption rates of these innovative formulations. Our goal is to deliver highly customized and effective development services that are meticulously tailored to the unique needs and expectations of our client base.

Why Develop Oral Nucleic Acid Formulations?

When taken orally, nucleic acid medications face challenges like stomach acidity, enzyme breakdown, and mucus barriers outside cells, along with obstacles like cellular membranes and entrapment within endosomes inside cells. To overcome these issues, strategies utilizing nanoparticles for oral delivery are developed. These systems provide protection against digestive degradation, enhance drug loading, allow flexibility for various nucleic acids, offer customizable sizes and shapes, target specific cells with modified compounds, and assist in crossing intestinal cell barriers.

Fig.1 Features of developing oral formulations.Fig.1 Characteristics of oral formulation development. (CD Formulation)

Explore our Oral Nucleic Acid Formulation Development Services

Development of Oral Nucleic Acid Drug Formulation Carriers

Items Descriptions
Extracellular Vesicles (EVs) Development EVs, including MEs, OMVs, and PEVs, are nano-sized vesicles that transport nucleic acids and facilitate cellular absorption by protecting their cargo from adverse environments.
Polymer Nanoparticles Development Cationic polymers like PEI and chitosan encapsulate nucleic acids via electrostatic attraction, enhancing their uptake and lysosomal escape, and can be tailored for specific targeting functions.
Lipid Nanoparticles (LNPs) Development LNPs, especially liposomes with cationic lipids, form bilayer-structured spheres engaging nucleic acids through electrostatic and hydrophobic interactions for efficient delivery.

Development of Oral Dosage Forms

  • Development of Oral Solid Nucleic Acid Formulations

Our oral solid nucleic acid formulation development services involve the utilization of innovative technologies, focusing on optimizing drug stability and absorption efficiency. These offerings include designing formulations, testing stability, and optimizing production to maintain consistent product quality in diverse conditions. Furthermore, experimenting with various excipients and production techniques can significantly improve the bioavailability of solid nucleic acid formulations.

  • Development of Oral Liquid Nucleic Acid Formulations

Our oral liquid nucleic acid formulation development services aim to provide highly precise and controlled nucleic acid delivery solutions. These services include formulation development of liquid dosage forms, selection of carrier systems, and regulation of solubility and viscosity to ensure stability and release characteristics of nucleic acids in the gastrointestinal tract. With modern analytical techniques and laboratory testing, the physicochemical stability and consistency of liquid formulations in different environments are ensured, thereby optimizing nucleic acid delivery efficiency.

Our Solutions for Oral Formulation Development

Solutions Descriptions
Chemical Modifications By modifying nucleic acid molecules, such as methylation or phosphorylation, enhance their stability in digestive environments.
Protective Mechanisms Develop protective coating or encapsulation technologies to prevent nucleic acid degradation in gastric fluids.
Targeted Delivery Incorporate bio-recognition molecules to ensure accurate transport and release of nucleic acids to target cells or tissues.
Permeability Enhancement Technologies Use chemical enhancers or mechanical methods (such as electroporation) to increase the permeability of nucleic acids through the intestinal epithelium.
Formulation Optimization Adjust the physical and chemical properties of formulations, such as particle size, surface charge, and solubility, to increase bioavailability.

Our Workflow for Oral Nucleic Acid Formulation Development

Fig.2 Diagram illustrating the process of creating oral nucleic acid formulations.Fig.2 Flow chart of oral nucleic acid formulation development. (CD Formulation)

  • Molecular Design and Construction

Design appropriate nucleic acid molecular structures based on target functions, synthesize or clone them, ensuring they possess the required characteristics.

  • Formulation Development

Design formulations, select suitable excipients, and optimize formulation stability and bioavailability to meet the requirements of oral administration.

  • Process Optimization and Scale-Up Production

Optimize production processes, determine key parameters, conduct small-scale pilot production, and evaluate scalability to support large-scale production.

  • Quality Assessment and Control

Develop detailed quality standards and conduct comprehensive testing of the physical, chemical, and biological properties to ensure the product meets quality requirements and industry standards.

Our Technology Platforms

Formulation Preparation Technologies

Technologies Descriptions
Solid Dispersion Preparation Technology The technology can be used to improve the solubility and bioavailability of nucleic acid drugs in oral routes.
Hot Melt Extrusion Technology The technology helps to uniformly disperse nucleic acid drugs into the matrix, improving stability and release characteristics.
Drug Nanocrystal Technology The technology is used to increase the solubility and absorption rate of nucleic acid drugs by reducing particle size.
Coating Technology The technology is typically used to protect nucleic acid drugs from the gastrointestinal environment and achieve controlled release.
3D Printing Technology The technology can be used to precisely customize different geometries and release characteristics, enhancing oral administration efficiency.
Microfluidics Technology Our technology assists in precise manipulation of nucleic acid drug preparation and processing at the microscale, suitable for high-throughput screening and small-batch production.

Characterization Technologies

  • Spectral Analysis - Includes UV-visible spectrophotometry, used for identifying the chemical composition of nucleic acids and their carriers.
  • DLS - Evaluates the size distribution and potential of carriers, which is crucial for understanding their stability and in vivo behavior.
  • TGA and DSC - Used to evaluate the thermal stability and interaction of formulation components.

Our Advantages of Oral Nucleic Acid Formulation Development

  • Utilizing various innovative formulation technologies, such as hot melt extrusion and microfluidics, can achieve more efficient and precise nucleic acid carrier construction.
  • Novel coating and nanotechnologies help to enhance the stability of nucleic acid molecules and their bioavailability in vivo.
  • Customizable development of suitable oral formulations according to different types of nucleic acids and application needs, adapting to diverse market demands.
  • Experts covering chemistry, materials science, and biotechnology provide comprehensive support, ensuring the effectiveness and innovation of the formulation development process.

Publication Data

Technology: Versatile OrD LNP formulation development platform for encapsulation and delivery of siRNAs and mRNAs

Journal: Drug Delivery and Translational Research

IF: 5.7

Published: 2024

Results:

This study introduces a multifunctional OrD LNP designed to deliver siRNAs and mRNAs. By adding cationic lipids to the LNP base, keeping total cationic and ionizable lipids at 50%, the formulation exhibits greater bile salt resistance. Tests highlight ionizable lipids' role in efficacy; 20% cationic and 30% ionizable lipids optimize performance. OrD LNP shows increased potency after exposure to various gastric and intestinal conditions. Confocal microscopy and flow cytometry confirm cellular uptake, with in vivo results proving successful delivery of siRNA and mRNA.

Fig.3 Administering stabilized lipid nanoparticles orally for nucleic acid treatments.Fig.3 Oral delivery of stabilized lipid nanoparticles for nucleic acid therapeutics. (Suri K, et al., 2024)

CD Formulation's professional team is fully prepared and ready to support your oral nucleic acid formulation development projects at any time, ensuring the smooth progress of your R&D endeavors. For additional information or to initiate a rewarding collaboration, please feel free to contact us and explore the possibilities together.

References

  1. Suri K, Pfeifer L, Cvet D, et al. Oral delivery of stabilized lipid nanoparticles for nucleic acid therapeutics. Drug Deliv. Transl. Res. 2024: 1-15.
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