What is bioavailability?Bioavailability Enhancement TechniquesEnhancing Bioavailability with SeraNovo

 

 

 

 

Bioavailability Enhancement

Increasing the Effectiveness of Medications

ENKR

Every time a patient takes medication, the expectation is clear – effectiveness in treating the condition.
However, the reality is not all medications are created equally. Some face a challenge known as low bioavailability, hindering their absorption in the body and compromising their efficacy. This is where bioavailability enhancement techniques step in – crucial processes dedicated to improving the absorption and overall effectiveness of medications.
SeraNovo is an expert in increasing the  bioavailability of medications, especially those for which traditional formulation strategies fail.

 

Learn more

Compared to traditional formulation techniques, we:

Develop formulations 60% faster

 

Clients benefit from rapid development and

answers about their molecular assets

Require 50% less API

 

With minimal active ingredient, we tailor

formulations to each molecule.

Save significant costs

 

One-step manufacturing means, easy scale-up and

reduced manufacturing costs

 

What is Bioavailability?

 

The relevance of bioavailability in drug development

Bioavailability is an important pharmacokinetic parameter and refers to the proportion of an active pharmaceutical ingredient (API or drug that is administered orally (by mouth)) and successfully absorbed into the bloodstream, where it can exert its intended therapeutic effect.

 

The Challenges of Oral Medication Absorption: Navigating Hurdle

When a medication is taken orally, it must pass through the digestive system before it can enter the bloodstream. However, there are various hurdles that can impede this process resulting in low bioavailability which means that the medication may not be as effective as it could be. Such hurdles include: 

⇒ Chemical and enzymatic degradation: Drugs can be broken down or metabolized by enzymes in the gastrointestinal tract or liver before they reach the bloodstream.

 

⇒ Poor permeability: Some drugs may not easily cross the intestinal wall due to their chemical structure or size, which can reduce their absorption into the bloodstream.

 

⇒ Drug-drug or drug-food interactions: Certain drugs or food components may interact with the drug, affecting its absorption, distribution, or metabolism.

⇒ Poor solubility: Some drugs have low solubility in the gastrointestinal fluids, which can limit their absorption across the intestinal wall.

 

⇒ First-pass metabolism: Some drugs are significantly metabolized in the liver during their first passage through the liver, reducing the amount of the active drug that reaches systemic circulation.

Quantifying oral bioavailability 

Oral bioavailability is usually expressed as a percentage or fraction of the administered dose that reaches systemic circulation. A drug with 100% oral bioavailability indicates that the entire administered dose is absorbed into the bloodstream and available to exert its therapeutic effect, while a drug with low oral bioavailability means that only a small portion of the dose is absorbed.


Bioavailability enhancement of poorly soluble drugs is important for several reasons:

⇒ Improved drug effectiveness: Enhancing the bioavailability of a drug allows more of the active pharmaceutical ingredient (API) to be absorbed into the bloodstream, leading to better therapeutic effects. This can lead to more effective treatment outcomes for patients, ensuring the intended therapeutic benefits are achieved.

 

⇒ Reduced dosage requirements: By increasing the bioavailability of a poorly soluble drug, the required dosage to achieve the desired therapeutic effect can be reduced. This can lower the risk of side effects and adverse reactions, making the drug safer for patients to take and improving overall patient compliance.

 

⇒ Cost-effectiveness: Improving drug bioavailability reduces dosage needs, enhances efficacy, and lowers costs for development and treatment, fostering affordability and accessibility for better healthcare outcomes.

⇒ Extended patent life: Improving the bioavailability of existing drugs can lead to the development of new formulations, which can extend the patent life of a drug. This enables pharmaceutical companies to continue generating revenue from their products, which can be reinvested into research and development of new therapies.

 

⇒ Rescue of failed drug candidates: Some drug candidates may have poor bioavailability, rendering them ineffective in clinical trials. Enhancing their bioavailability can help rescue these drug candidates, potentially turning them into successful, marketable medications.

 

⇒ Environmentally friendly: Bioavailability enhancement can reduce the amount of API required for a therapeutic effect, leading to decreased waste and a reduced environmental impact.

 

Bioavailability Enhancement Techniques

 

Various techniques can be employed to improve the bioavailability of poorly water-soluble molecules.

Some of the commonly used methods are:

Particle Size Reduction Systems

Nanosuspensions play a crucial role as a drug delivery system by utilizing small particles, typically falling within the 10-500 nanometer range. This approach aims to improve the solubility and bioavailability of poorly water-soluble drugs.

 

Key Features:

  • Particle Size: Nanosuspensions employ small particles with a larger surface area to volume ratio, facilitating enhanced dissolution and absorption in the body.
  • Preparation Methods:
    • High-Pressure Homogenization
    • Media Milling
  • Stabilization Techniques:
    • Surfactants
    • Polymers

Advantages:

Challenges:

Promising results in enhancing drug efficacy

Cumbersome production method

Reduction in required dosage, leading to improved patient outcomes

Physical instability of nanoparticles over time (aggregation)
Decreased drug toxicityNecessity of an aqueous vehicle

 

Diagram representation of particle size reduction

Lipid-Based Delivery Systems

Lipid-Based Formulations (LBFs) are a specialized drug delivery system leveraging lipids and lipophilic excipients to optimize the solubility and bioavailability of lipophilic drugs.

 

Formulation Structure:

  • Consists of a lipid vehicle in which the drug is dissolved
  • Presence of surfactants determines the drug release mechanism

 

Surfactant Presence:

  • No Surfactants:
    • Drug release occurs as the lipid vehicle is digested by intestinal lipases
    • Effectively addresses food-effects
  • With Surfactants:
    • Lipid vehicle dispersed in nano- or micro-sized droplets
    • Facilitates absorption, particularly influenced by gastric- and intestinal fluid volume and pH
Advantages:Challenges:

Demonstrates effectiveness in combatting food-effects

Higher dependency on gastric- and intestinal fluid conditions
Addresses solubility and bioavailability challenges in lipophilic drugsMajor limitation: Low drug load achievable with most poorly soluble APIs

 

 

Diagram representation of a Lipid-Based Delivery System

Solid Form Manipulation Systems

Amorphous Solid Dispersions (ASDs) represent a sophisticated drug delivery system incorporating poorly water-soluble drugs into a polymer matrix in an amorphous state.

 

Formulation Structure:

  • Incorporates poorly water-soluble drug into a polymer matrix
  • Utilizes the amorphous state for enhanced drug solubility and bioavailability
  • ASDs designed to release the drug in a controlled manner

 

Amorphous vs. Crystalline Form:

Amorphous form has a higher energy state

More easily dissolved in water compared to the crystalline form

 

Preparation Methods:

Various Techniques:

  • Spray drying
  • Hot melt extrusion
  • Solvent evaporation

Diagram representation of amorphous solid dispersion

AdvantagesChallenges
Improved drug solubility and bioavailabilityPhysical and chemical stability issues
Controlled release mechanismPotential impact on shelf life and performance

How SeraNovo’s formulations enhance bioavailability

 

Experience rapid development and minimal API usage 

 

Our innovative liquid formulation technology platforms like HyDES and LiDES overcome solubility and permeability limitations of APIs. Our supersaturated solutions are stabilized by carefully chosen excipients, which we expertly screen using minimal amounts of API and limited time. The screening is rapid and can be done on small scales, giving us an edge in development speed and efficiency. Experience the benefits of our advanced liquid formulation technology and achieve greater drug efficacy and patient outcomes.

 

Experience the same benefits with our Solid HyDES Platform

 

The Solid HyDES platform engineers a dehydrated solid (glass) powder, utilizing a screening method similar to that used for liquid platforms, ensuring swift screening on small scales. Upon ingestion, the formulation effortlessly rehydrates, enabling quick dissolution, heightened bioavailability, and consequently fostering increased drug absorption.

 

 

Learn more about our technology platforms:

 

HyDES      Solid HyDES      LiDES      PeptiDES

 

Back to top