Liposomes for Oral Drug Delivery

Introduction to Our Liposomal Transdermal Drug Delivery System Development

Oral drug delivery remains the most preferred and patient-compliant route of administration. However, the bioavailability of many therapeutics—especially peptides, proteins, poorly water-soluble drugs, and biologics—is severely limited by harsh gastrointestinal (GI) conditions, enzymatic degradation, and low permeability across intestinal barriers. Liposomal drug delivery systems, with their bilayer vesicular architecture and biomimetic properties, offer a transformative strategy to overcome these challenges. BOC Sciences provides an advanced Liposomal Oral Drug Delivery System Development Service, leveraging decades of expertise in lipid-based nanocarrier technologies. Our offerings are strictly focused on preclinical-stage development, encompassing liposome design, optimization, analytical characterization, and in vitro/in vivo evaluations to accelerate oral drug delivery innovations.

How to Get Started with Us?

Begin by reaching out to us through our website or via email to initiate a consultation for your liposomal oral drug delivery system development needs.
Schedule an initial meeting where our experts will discuss your project's specific goals, requirements, and therapeutic targets.
Our team will assess the feasibility of your liposomal drug delivery system and provide initial insights and recommendations.
We will present a comprehensive development plan that includes a clear timeline, estimated budget, and key project milestones to ensure a structured approach.
Once both parties agree on the terms, a formal contract will be signed, officially kick-starting the development process.

Inquire today to accelerate your vaccine development.

Request A Quote

Price Inquiry

What are the Methods of Oral Drug Delivery?

Conventional Oral Tablets and Capsules

Widely used but often limited by drug solubility, GI degradation, and first-pass metabolism.
Unsuitable for peptide, protein, and nucleic acid drugs without advanced formulation strategies.

Microparticle and Nanoparticle Delivery Systems

Enhance surface area and protect drugs from acidic pH.
Often lack precise control over release kinetics and mucosal permeability.

Self-emulsifying Drug Delivery Systems (SEDDS)

Improve solubility but can be unstable in bile salt-rich environments.

Liposomal Systems (BOC Sciences' Focus)

Liposomes offer targeted and sustained drug release, protect actives from degradation, and can exploit transcellular and paracellular absorption pathways.
Especially suited for encapsulating hydrophilic, hydrophobic, and amphiphilic drugs.

Comprehensive Services for Liposomal Oral Drug Delivery System Development

BOC Sciences offers a robust and comprehensive range of services tailored to the development and optimization of liposomal oral drug delivery systems. We are committed to addressing the unique challenges associated with oral drug delivery, such as poor solubility, low bioavailability, and instability in the gastrointestinal tract. Our expert team leverages cutting-edge technology platforms and extensive industry experience to support the successful development of oral liposomal systems for various types of drugs.

Custom Liposome Types for Oral Delivery

We provide tailored liposome formulations that are optimized for the oral delivery of your drug. Depending on the physicochemical properties of your active pharmaceutical ingredient (API), we can select the most appropriate liposome type, including:

Conventional Liposomes (CLs): Designed for simple drug encapsulation with passive loading methods, ideal for hydrophilic and moderately lipophilic drugs.
PEGylated Liposomes: Using polyethylene glycol (PEG) coatings to enhance stability, reduce premature immune recognition, and improve the circulation time of the liposomes, especially for drugs requiring systemic delivery.
Stealth Liposomes: Designed to avoid rapid clearance by the reticuloendothelial system (RES) and prolong the drug's residence time in circulation for improved therapeutic outcomes.
Targeted Liposomes: Incorporating surface modifications, such as ligands or antibodies, to target specific receptors within the gastrointestinal mucosa, enhancing drug absorption at the site of action.
Stimuli-Responsive Liposomes: These liposomes are engineered to release their drug cargo in response to changes in environmental conditions, such as pH or temperature, ensuring targeted and controlled release within the GI tract.

Liposome Drug Encapsulation and Loading Optimization

Our services encompass advanced techniques to maximize the efficiency and stability of drug encapsulation:

Hydrophilic Drug Loading: We use passive encapsulation methods such as thin-film hydration or reverse-phase evaporation for water-soluble drugs. We also employ active loading strategies like pH-gradient or ammonium sulfate gradients to enhance drug loading efficiency.
Hydrophobic Drug Loading: Lipophilic drugs, such as poorly water-soluble small molecules, are incorporated through solvent evaporation techniques and can be entrapped within the lipid bilayer for controlled release.
Dual-Drug Loading: For combination therapies, we optimize the loading of two or more drugs into the same liposomal vehicle, maintaining stability, appropriate release rates, and synergistic effects.

In Vitro and Ex Vivo Testing for Liposomal Oral Delivery

Testing the functionality and effectiveness of liposomal formulations is a critical step in preclinical development. BOC Sciences offers robust in vitro and ex vivo testing services to ensure that liposomal oral drug delivery systems perform as expected:

Gastrointestinal Stability Testing: Simulated gastrointestinal conditions (including simulated gastric fluid (SGF) and simulated intestinal fluid (SIF)) are used to assess liposome stability and drug release profiles under acidic, neutral, and alkaline conditions that mimic the human GI tract.
Enzymatic Degradation Studies: Liposomes are exposed to digestive enzymes (such as pepsin and lipase) to evaluate the stability of the lipid bilayer and encapsulated drug under digestive conditions.
Intestinal Permeability Studies: Using Caco-2 cell monolayers or Ussing chambers, we evaluate the permeation of liposomal drugs through the intestinal epithelium, providing insights into the bioavailability and absorption potential of the formulation.
Mucosal Interaction Studies: Liposomes are assessed for their interaction with the intestinal mucus layer, which is critical for determining the potential for drug absorption and the ability to cross the epithelial barrier.

Step-by-Step Process of Liposomal Oral Drug Delivery System Development

1. Feasibility and Physicochemical Profiling

Analysis of drug solubility, logP, pKa, and stability under gastric/intestinal pH.
Determination of optimal lipid:drug molar ratios for encapsulation.

2. Liposome Design and Prototyping

Selection of lipid types (e.g., DSPC, cholesterol, DOTAP) tailored to the drug's properties.
Fabrication via thin-film hydration, ethanol injection, or microfluidic mixing.

3. Encapsulation Efficiency and Size Control

Optimization to reach >90% encapsulation for hydrophobic APIs.
Uniformity control via dynamic light scattering (DLS) and polydispersity index (PDI).

4. GI Stability and Mucus Penetration Assays

Evaluation under simulated gastric and intestinal fluids (SGF, SIF).
Particle transport across mucin gels or mucosal epithelial monolayers.

5. In vitro Absorption and Permeability Testing

Caco-2/HT29-MTX co-culture systems for better intestinal mimicry.
Transwell permeability studies and Papp coefficient determination.

6. Lyophilization or Spray-Drying for Oral Form Compatibility

Converting liposomal suspension into powder or granule formats.
Preservation of vesicle integrity post-redispersion.

7. Process Transfer and Scale-Up

Reproducibility across scale.
Optimization for lyophilized or capsule formulations.

Benefits of Our Liposomal Oral Drug Delivery System Development

Deep Technical Expertise in Lipid-Based Drug Delivery: With over two decades in biopharmaceutical formulation, BOC Sciences brings precision-driven innovation to each project. Our in-depth understanding of lipid behavior in gastrointestinal environments ensures high-performing oral liposomal systems.
Tailor-Made Liposome Platforms: Each formulation is engineered based on your molecule's physicochemical profile and absorption challenge—whether that's a hydrophobic small molecule or an acid-sensitive peptide.
Proven Success Across Molecule Classes: Our oral liposomal systems have successfully encapsulated siRNA, antibiotics, cannabinoids, and anti-cancer compounds, demonstrating substantial improvements in bioavailability in simulated models.
Integrated Analytical & Regulatory Support: We provide full documentation for preclinical regulatory submissions, including full physicochemical characterization, in vitro release, and GI stability data packages.

Applications of Our Liposomal Oral Drug Delivery System Development

Liposomal oral drug delivery platforms have emerged as a transformative technology for overcoming the limitations of traditional oral formulations. At BOC Sciences, our liposomal systems have been engineered to support a broad range of therapeutic applications, each with unique biopharmaceutical challenges that demand precision-designed lipid carriers.

Oral Delivery of Peptides and Proteins

Peptide- and protein-based therapeutics face rapid enzymatic degradation in the GI tract and poor transcellular transport. Liposomal encapsulation provides a protective microenvironment that:

Shields biologics from gastric and proteolytic enzymes.
Enhances mucosal adhesion and facilitates paracellular transport via lipid-mediated membrane fusion.
Enables sustained release and site-specific delivery in the small intestine.

Use Case: Liposomal delivery of insulin analogs and GLP-1 receptor agonists for oral antidiabetic formulations.

Enhancement of Bioavailability for Poorly Soluble APIs

Many promising small-molecule drugs are severely limited by poor aqueous solubility and extensive first-pass metabolism. Liposomes improve their solubilization, protect against premature degradation, and can promote lymphatic uptake to bypass hepatic clearance.

Use Case: Oral delivery of cannabinoids, antifungals (e.g., itraconazole), or anticancer compounds like paclitaxel and curcumin analogs with enhanced systemic exposure.

Site-Targeted GI Delivery in Inflammatory Disorders

Liposomal formulations engineered with pH-sensitive or enzyme-responsive coatings can enable localized drug release in specific regions of the GI tract. This approach is particularly valuable for conditions like:

Inflammatory Bowel Disease (IBD): Liposomes protect anti-inflammatory drugs (e.g., corticosteroids, 5-ASA) until they reach inflamed colonic tissues.
Colorectal Cancer: Tumor-targeted liposomes carrying chemotherapeutic agents selectively release drugs in malignancy-associated microenvironments.

Oral Delivery of Nucleic Acids and Gene Therapeutics

Nucleic acid drugs such as siRNA, antisense oligonucleotides, and mRNA are highly sensitive to nuclease degradation and poorly absorbed via oral routes. Liposomal carriers provide:

Protection against enzymatic hydrolysis.
Enhanced intracellular delivery through endocytosis pathways.
Opportunities for functionalization with ligands for receptor-mediated uptake.

Use Case: Oral mRNA vaccine delivery, siRNA therapy for intestinal epithelial targets, and gene-editing payloads delivered via non-viral vectors.

Oral Liposomal Vaccines and Immunotherapeutics

Liposomal vesicles mimic pathogen-associated lipid bilayers and can function as adjuvants or delivery vehicles for oral vaccine strategies. These systems enhance antigen stability and mucosal immune activation, enabling:

M cell-mediated transcytosis in Peyer's patches.
Stimulated IgA secretion and systemic immunity via gut-associated lymphoid tissues (GALT).

Use Case: Oral vaccines for viral or bacterial pathogens, mucosal immunotherapy, and tolerogenic oral vaccine delivery for autoimmune disease modulation.

Neurological and CNS Drug Delivery via the Gut-Brain Axis

Emerging studies suggest the GI tract plays a regulatory role in CNS signaling. Liposomal oral delivery offers a route to target neuroactive compounds that modulate the gut-brain axis, delivering drugs that might otherwise be degraded or poorly absorbed.

Use Case: Delivery of neuropeptides, nootropics, or mood stabilizers for neurodegenerative or neuropsychiatric disorders with enhanced oral bioavailability.

FAQs – Insights about Our Liposomal Oral Drug Delivery System Development

What types of drugs are suitable for oral liposomal delivery? Drugs that are poorly water-soluble, sensitive to gastric or enzymatic degradation, or have poor membrane permeability benefit significantly from liposomal encapsulation. These include peptides, hydrophobic small molecules, and gene-based therapies.
How stable are your oral liposomes in gastrointestinal conditions? We use advanced lipid compositions and protective coatings to engineer liposomes that can withstand acidic pH, bile salts, and digestive enzymes. For acid-labile APIs, we offer enteric-coating or bile salt-resistant liposomes to ensure payload protection through the stomach and targeted release in the intestine.
Can you assist with transforming liposomal suspensions into oral solid dosage forms? Yes. We offer lyophilization, spray-drying, and granulation solutions to convert liquid liposomal formulations into stable powders, granules, or capsules, preserving the vesicle integrity and drug stability for oral delivery.
How do you evaluate whether the liposomes are effectively absorbed in the intestine? We conduct rigorous in vitro permeability studies using Caco-2 and mucus-secreting co-cultures, as well as ex vivo intestinal models. These allow us to simulate and quantify the extent of GI absorption, ensuring your formulation has strong preclinical performance metrics before animal studies.

For customized solutions in liposomal oral drug delivery system development, contact BOC Sciences to leverage our expertise and innovation in transforming your molecule into a clinically viable oral therapy.

Supplementary Knowledges: Oral Drug Delivery

What are the advantage and disadvantage of oral drug delivery?

Advantages of oral drug delivery include high patient compliance, ease of administration, and cost-effectiveness. It eliminates the need for sterile procedures and enables outpatient treatment. However, disadvantages include variable bioavailability due to first-pass metabolism, enzymatic degradation in the gastrointestinal tract, and limited absorption of poorly soluble or unstable compounds.

How are oral drugs distributed?

After oral administration, drugs are absorbed primarily through the gastrointestinal (GI) mucosa into the portal circulation. From there, they undergo first-pass metabolism in the liver before entering systemic circulation. The extent and rate of distribution depend on the drug's physicochemical properties, plasma protein binding, and tissue permeability.

Oral nanoparticle drug delivery

Oral nanoparticle drug delivery involves encapsulating active pharmaceutical ingredients within nanocarriers—such as liposomes, polymeric nanoparticles, or solid lipid nanoparticles—to enhance stability, solubility, and absorption. These systems protect the drug from degradation in the GI tract, facilitate mucosal penetration, and can improve the bioavailability of poorly absorbed compounds.

Liposomal Oral Drug Delivery System Development Service