Advancing Drug Delivery with Optizorb Technology: A Review of Mechanisms, Formulation Strategies, and Benefits

A revolutionary development in the pharmaceutical sector, Optizorb technology was created especially to improve the efficacy and administration of painkillers, especially paracetamol. By greatly increasing the breakdown and absorption rates of conventional paracetamol formulations, this cutting-edge technology overcomes their drawbacks and produces pain relief more quickly.

Table 1: The Comparison between Optizorb Technology and Traditional methods.

Optizorb technology is a proprietary delivery system used in the formulation of pharmaceutical tablets, designed to improve the bioavailability and absorption of active pharmaceutical ingredients (APIs). The technology is particularly important in oral drug formulations, where maximizing the bioavailability of the active ingredient ensures better therapeutic outcomes.

Overview of Optizorb Technology

Optizorb technology involves the use of special excipients and formulations that enhance the solubility and absorption of poorly soluble drugs. By improving the dissolution rate of the drug in the gastrointestinal tract, Optizorb ensures that the active ingredient is available for absorption in a more efficient and rapid manner. This helps in achieving therapeutic levels of the drug more effectively. The system is commonly employed in solid oral dosage forms like tablets and capsules. With this technology, the formulation is able to "optimize" the release of the drug, making it more bioavailable to the body, and improving its clinical efficacy.

How Optizorb Technology Works

The basic principle behind Optizorb technology lies in enhancing the dissolution of the active ingredient in the gastrointestinal fluid. This is achieved through a combination of techniques, such as:

1. Particle Size Reduction: The technology utilizes processes that reduce the particle size of the drug, which significantly increases the surface area of the API. This increases the dissolution rate, as smaller particles tend to dissolve faster.
2. Use of Solubilizing Agents: Special excipients are incorporated into the formulation, which act as solubilizers. These agents help the poorly water-soluble drug to dissolve more readily in the stomach, facilitating easier absorption.
3. Controlled Release: In some cases, Optizorb technology may also enable a controlled release of the active ingredient over time, ensuring a more consistent and sustained therapeutic effect.
4. Improved Bioavailability: With improved dissolution and solubilization of the drug, the active ingredient can be absorbed more efficiently into the bloodstream, thereby increasing its bioavailability. This is particularly valuable for drugs that are poorly absorbed through the gastrointestinal tract.

Benefits of Optizorb Technology in Tablets

1. Enhanced Drug Absorption: The primary benefit of Optizorb technology is improved absorption of the drug. By increasing the rate and extent to which the drug dissolves, more of the drug reaches systemic circulation, enhancing its therapeutic effects.
2. Improved Bioavailability: Many drugs have low bioavailability due to poor solubility. Optizorb technology helps overcome this limitation, enabling better absorption and achieving the desired therapeutic effect.
3. Faster Onset of Action: With enhanced dissolution and solubility, drugs formulated with Optizorb technology may have a faster onset of action, improving patient outcomes, particularly in cases where quick therapeutic response is needed.
4. Reduced Dosage Requirements: Improved bioavailability may also mean that lower doses of the drug are required to achieve the desired therapeutic effect. This can reduce the risk of side effects and improve patient compliance.
5. Formulation Flexibility: Optizorb technology allows for more flexibility in drug formulation. It can be applied to a variety of drugs, including those with challenging solubility profiles. This makes it a versatile solution for many pharmaceutical products.

Mechanism Of Action

The mechanism of action of tablets formulated with Optizorb technology centers around improving the solubility and absorption of active pharmaceutical ingredients (APIs) that are typically poorly soluble in water or in the gastrointestinal tract. These tablets are designed to optimize the release and absorption of the drug, thereby enhancing its therapeutic efficacy. Below is an in-depth explanation of how Optizorb technology functions in the body.

1. Enhancing Solubility and Dissolution

Many drugs, especially those that are poorly soluble, face challenges in dissolving effectively in the gastrointestinal fluids, which limits their absorption and bioavailability. Optizorb technology is specifically designed to address this issue by improving the solubility and dissolution rate of such drugs.

• Particle Size Reduction: One of the key strategies used by Optizorb technology is reducing the size of the active ingredient’s particles. By reducing the particle size, the surface area of the drug increases, allowing it to dissolve more easily in the aqueous environment of the gastrointestinal tract.
• Use of Solubilizing Agents: Optizorb technology often incorporates special excipients known as solubilizers, which are substances that help dissolve poorly soluble drugs. These solubilizers can form micelles or complexes with the drug molecules, making them more water-soluble and enabling their dissolution in the stomach or intestines.
• Hydrophilic Matrix or Coating: Some formulations may include a hydrophilic matrix or coating that attracts water, further aiding the dissolution of the drug in the aqueous environment of the gastrointestinal tract. This allows for a faster and more efficient release of the active pharmaceutical ingredient.

2. Improved Absorption

Once the drug is dissolved in the gastrointestinal fluids, it needs to be absorbed through the lining of the intestines into the bloodstream. Optizorb technology helps improve the absorption of drugs by:

• Increased Surface Area: By reducing particle size, Optizorb formulations increase the surface area of the drug, which improves its interaction with the gastrointestinal fluids and enhances absorption across the intestinal wall.
• Facilitating Membrane Penetration: Some Optizorb formulations may also include excipients that help the drug molecules cross the gastrointestinal membrane more easily. This can include compounds that enhance the permeability of the intestinal wall, allowing the drug to enter the bloodstream more effectively.
• Enhanced Diffusion: As the drug dissolves quickly, it is in its molecular form for a longer period in the digestive tract. This prolonged molecular phase allows for greater diffusion and absorption into the bloodstream.

3. Bioavailability Optimization

Bioavailability refers to the proportion of the drug that enters the circulation and is available to have a therapeutic effect. Optizorb technology directly influences bioavailability in several ways:

• Faster Dissolution: The quicker the drug dissolves, the quicker it can be absorbed, which leads to a higher bioavailability. Since poorly soluble drugs tend to dissolve slowly, their bioavailability is often limited. Optizorb enhances dissolution, ensuring that the drug reaches therapeutic levels faster.
• Higher Plasma Concentration: The improved dissolution and absorption lead to a higher plasma concentration of the drug. This ensures that the active ingredient is available in the bloodstream in sufficient amounts to exert its therapeutic effects.
• Consistent Absorption: By optimizing the solubility and release rate of the drug, Optizorb technology contributes to more consistent absorption across different individuals. This is especially important for drugs with high variability in absorption, where variations in bioavailability could affect their effectiveness.

4. Controlled or Modified Release (in Some Formulations)

Some Optizorb formulations incorporate elements of controlled release or modified release. This ensures that the drug is released at a steady rate over time, which can offer several benefits:

• Sustained Action: The controlled release of the drug can help maintain therapeutic levels of the drug in the bloodstream for an extended period. This minimizes the need for frequent dosing and helps maintain consistent therapeutic effects.
• Reduced Side Effects: By reducing peak plasma concentrations and promoting a steady release, the controlled release formulation may also help to reduce potential side effects that arise from large spikes in drug concentrations.
• Localized Delivery: Some Optizorb formulations can also be tailored to release the drug at specific locations in the gastrointestinal tract, enhancing the drug’s action at its site of absorption or where it exerts its therapeutic effects.

5. Minimizing Drug Degradation

For some drugs, degradation or instability in the acidic or enzymatic environment of the stomach can occur. Optizorb technology can help prevent this degradation by ensuring that the drug is solubilized before it encounters conditions that might degrade it, allowing for better preservation of the drug's integrity.

Mechanism of Action of Alginic Acid

Alginate acid (or alginate), derived from brown seaweed, plays a crucial role in Optizorb technology due to its unique properties that help enhance the solubility, bioavailability, and controlled release of poorly soluble active pharmaceutical ingredients (APIs). In Optizorb formulations, alginic acid can be used in various ways to optimize the drug delivery process. Here’s how alginate works within Optizorb technology and its mechanism of action:

1. Improvement of Drug Solubility (Solubilizing Effect)

Alginic acid has the ability to improve the solubility of poorly water-soluble drugs, which is a significant advantage for drugs that have low bioavailability due to poor solubility.

• Mechanism: Alginic acid is a hydrophilic (water-attracting) polymer, and when incorporated into the tablet formulation, it helps solvate the poorly soluble drug in the gastrointestinal tract. Upon contact with water or digestive fluids, alginate can increase the dissolution rate of the drug by improving its interaction with water, making the drug dissolve faster and allowing it to be absorbed more efficiently.
• Benefit: This solubilizing effect is particularly useful for BCS Class II and Class IV drugs (those with low solubility but high permeability), as it helps overcome the solubility barriers, leading to enhanced bioavailability.

2. Gelation in the Stomach (Mucoadhesion)

Alginate can also interact with the mucosal lining of the stomach and intestines, which plays a role in mucoadhesion. This interaction may increase the retention time of the tablet in the gastrointestinal tract, potentially improving the absorption of the drug.

• Mechanism: Alginate forms a viscous gel upon contact with the stomach's acidic environment, which can adhere to the mucus layer of the stomach and intestines. This increases the residence time of the formulation at the absorption site, allowing for extended contact with the mucosal lining, which can improve absorption.
• Benefit: Mucoadhesion prolongs the drug's contact with the absorption sites in the stomach and small intestine, potentially enhancing the overall bioavailability of the drug.

3. Protective Barrier Against Degradation

For some drugs that are sensitive to acidic environments or enzymatic degradation in the gastrointestinal tract, alginic acid can help protect the drug from early degradation, especially in the stomach.

• Mechanism: When alginate forms a gel, it can act as a protective barrier around the active ingredient, shielding it from the harsh acidic environment of the stomach. This is particularly beneficial for drugs that are unstable in acidic conditions or those that undergo degradation due to the enzymatic environment in the stomach or intestines.
• Benefit: This protective barrier ensures that the API remains intact and effective until it reaches more favorable environments, such as the small intestine, where absorption can occur more effectively.

4. Regulation of pH in the Gastrointestinal Tract

Alginate is often used in conjunction with other excipients that help regulate the pH environment of the gastrointestinal tract. This can further enhance drug solubility, especially for drugs that are highly pH-sensitive.

• Mechanism: Alginate can buffer and help maintain an optimal pH in the digestive system, preventing drug degradation and improving solubility. For example, alginate can reduce the acid levels in the stomach, creating a more neutral or slightly alkaline environment that is better for dissolving certain drugs.
• Benefit: This buffering capacity ensures that the active ingredient is presented in a more favorable environment, potentially increasing the dissolution rate and bioavailability.

5. Reduction of Gastric Irritation

Alginic acid has been used in antacid formulations due to its ability to form a gel-like barrier that can protect the stomach lining from irritation caused by acidic environments. This property can be beneficial for drugs that might irritate the stomach, as alginic acid can help buffer the acidity and reduce the potential for gastric discomfort.

Mechanism: The gel formed by alginate creates a protective barrier that shields the stomach lining from excess acid, which may reduce irritation or discomfort associated with certain medications.

Benefit: By reducing gastric irritation, alginate can improve patient compliance, particularly for drugs that require long-term use or are known to cause stomach upset.

Mechanism of Action of Calcium Carbonate

Calcium carbonate is a versatile excipient used in Optizorb technology, primarily known for its role in enhancing the solubility, dissolution, and bioavailability of poorly soluble drugs. It also contributes to controlled release, drug protection, and improved patient experience. Here's how calcium carbonate works within the context of Optizorb technology:

1. pH Modulation and Drug Solubility Enhancement

One of the key mechanisms by which calcium carbonate works in Optizorb technology is through its ability to modulate the pH in the gastrointestinal tract. Many drugs have low solubility in acidic environments, particularly in the stomach, which can limit their absorption and bioavailability. Calcium carbonate can help overcome this challenge by neutralizing gastric acid and creating a more favorable environment for drug dissolution.

• Mechanism: When calcium carbonate is ingested, it reacts with the hydrochloric acid (HCl) in the stomach to form calcium chloride, carbon dioxide, and water. This reaction reduces the acidity (increases pH), creating a less acidic environment that may improve the solubility of certain drugs, especially those that are poorly soluble in acidic conditions.

CaCO3 (s)+2 HCl (aq)→ CaCl2 (aq)+CO2 (g)+H2O (l)\text{CaCO}_3 \, (s) + 2 \, \text{HCl} \, (aq) \rightarrow \, \text{CaCl}_2 \, (aq) + \text{CO}_2 \, (g) + \text{H}_2\text{O} \, (l)CaCO3?(s)+2HCl(aq)→CaCl2?(aq)+CO2?(g)+H2?O(l)

• Benefit: By reducing acidity, calcium carbonate helps increase the solubility of drugs that are pH-sensitive or have low solubility in acidic conditions. This results in faster dissolution and improved bioavailability, especially for drugs that may otherwise precipitate in the acidic environment of the stomach.

2. Facilitating Faster Drug Dissolution and Absorption

For many poorly soluble drugs, the rate of dissolution is the rate-limiting step in their absorption. By modifying the stomach’s pH, calcium carbonate can facilitate a faster dissolution of these drugs, leading to more rapid absorption into the bloodstream.

• Mechanism: The neutralizing effect of calcium carbonate on stomach acid can increase the solubility of the drug, leading to a faster rate of dissolution in the gastric fluids. As a result, the drug remains in a dissolved state for a longer period of time, which enhances its absorption in the small intestine.
• Benefit: The faster dissolution and subsequent absorption of the drug can lead to improved bioavailability, allowing the active pharmaceutical ingredient (API) to reach therapeutic levels in the bloodstream more efficiently and more quickly.

Enhancing Stability of the Formulation

Calcium carbonate can help maintain the stability of the drug formulation by acting as a buffering agent, particularly for drugs that are sensitive to pH changes. Some drugs degrade when exposed to highly acidic or highly basic environments, and calcium carbonate helps to maintain a stable pH, preventing premature degradation.

• Mechanism: By buffering the pH in the stomach and controlling the acidity, calcium carbonate helps maintain a consistent pH environment that is less likely to cause degradation or instability of the active ingredient.
• Benefit: This protective action ensures that the drug remains intact and effective throughout the gastrointestinal tract, leading to increased stability and bioavailability.

3. Gastrointestinal Comfort and Irritation Reduction

Calcium carbonate can also help reduce gastric irritation that some drugs may cause, particularly those that are acidic or can irritate the stomach lining. By neutralizing gastric acid, calcium carbonate can minimize the discomfort or irritation that might otherwise occur upon ingestion of certain drugs.

• Mechanism: Calcium carbonate neutralizes excess stomach acid, which not only improves drug solubility but also reduces gastric discomfort caused by acid-related conditions such as heartburn or gastritis.
• Benefit: This makes calcium carbonate particularly useful in formulations where patient comfort is important, enhancing patient compliance and ensuring that the drug can be taken without discomfort.

4. Buffering and Maintaining Drug Integrity

Calcium carbonate also serves as a buffering agent that helps to maintain the integrity of the formulation, particularly for drugs that are sensitive to environmental conditions like pH fluctuations, moisture, or temperature.

• Mechanism: By acting as a buffer, calcium carbonate can help stabilize the formulation and prevent any reactions that might occur between the drug and excipients, especially in the presence of moisture or acidic conditions.
• Benefit: This stabilization ensures that the drug maintains its potency, effectiveness, and safety throughout its shelf life.

Mechanism of Crospovidone

Crospovidone is a commonly used excipient in pharmaceutical formulations, especially in Optizorb technology, where it plays a critical role in enhancing drug solubility, dissolution rates, and bioavailability. As a superdisintegrant, crospovidone helps improve the rate of tablet disintegration and can be crucial in the controlled release and efficient absorption of the drug in the gastrointestinal tract. Below is an explanation of its mechanism of action in Optizorb technology:

1. Disintegration and Drug Release Enhancement

Crospovidone is primarily known for its ability to act as a superdisintegrant, which means it facilitates the rapid breakup or disintegration of tablets once they come into contact with water or gastric fluids.

• Mechanism: Upon contact with water, crospovidone swells and absorbs water rapidly, leading to the tablet's breakup. This allows the active pharmaceutical ingredient (API) to be released into the gastrointestinal tract more efficiently. Crospovidone’s unique structure, made up of cross-linked polyvinylpyrrolidone (PVP), helps in water uptake and tablet disintegration by rapidly swelling, which generates an internal force that breaks the tablet into smaller particles.
• Benefit: The faster disintegration of the tablet leads to quicker dissolution of the drug, ensuring faster release and more efficient absorption of the API in the gastrointestinal tract. This is especially important for poorly soluble drugs that may otherwise dissolve too slowly or incompletely.

2. Improved Drug Solubility and Bioavailability

Poorly soluble drugs often face challenges with bioavailability because their slow or incomplete dissolution limits their absorption. Crospovidone aids in overcoming these challenges by improving the rate of dissolution and increasing the surface area of the active drug exposed to the absorption sites.

• Mechanism: Crospovidone, by promoting rapid disintegration and swelling, increases the surface area available for dissolution. This allows more of the drug to dissolve quickly in the gastrointestinal fluids, enhancing its bioavailability. It helps in ensuring that the drug remains in solution form for a longer period, preventing premature precipitation or crystallization, which could hinder absorption.
• Benefit: This mechanism leads to enhanced drug solubility and faster dissolution rates, particularly for poorly soluble drugs (e.g., BCS Class II drugs), thereby improving their overall bioavailability.

3. Absorption Enhancement in the Gastrointestinal Tract

Crospovidone’s ability to enhance disintegration and dissolution also contributes to improving the drug’s absorption in the gastrointestinal tract.

• Mechanism: As crospovidone rapidly disintegrates the tablet, it exposes the drug to a larger surface area, which facilitates better contact with the gastrointestinal fluids. This increases the likelihood that the drug will be absorbed more efficiently in the small intestine, where the majority of drug absorption occurs.
• Benefit: This improves the overall bioavailability of the drug, particularly for those that would otherwise have difficulty dissolving in the stomach or intestines.

4. Increased Stability of the Formulation

Crospovidone can also help maintain the physical and chemical stability of the drug formulation by preventing moisture-induced degradation or clumping during storage and handling.

• Mechanism: Crospovidone has desiccant properties, meaning it can help absorb excess moisture in the formulation. This helps prevent hygroscopic excipients or active ingredients from absorbing water, which could lead to degradation or instability in the tablet.
• Benefit: By maintaining the stability of the formulation, crospovidone contributes to ensuring the long-term effectiveness and shelf-life of the drug product.

5. Mucoadhesion for Site-Specific Drug Delivery

Crospovidone, being a polymer, may also contribute to mucoadhesion in some cases, meaning it can adhere to the mucosal surfaces of the gastrointestinal tract, particularly in the small intestine. This can extend the time the drug remains in the absorption site.

• Mechanism: When crospovidone is used in certain formulations, it can help the drug stay in contact with the mucosal layer longer, promoting extended absorption and possibly reducing the frequency of dosing.
• Benefit: Mucoadhesion can improve the efficiency of drug absorption, particularly for drugs that require longer residence time in the gastrointestinal tract for optimal absorption.

Table 2: Combination Of Alginic Acid, Calcium Carbonate, Crospovidone as Super Disintegrants

Formulation Considerations

Table 3: The desired ratios of Alginic Acid, Calcium carbonate and Crospovidone