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Drug Formulation Whitepaper

Unique Formulation Opportunities for Drug Manufacturers

As drug manufacturers are acutely aware, formulating a product is not just about identifying the appropriate pharmaceutical ingredients and manufacturing processes; it is also about identifying the optimal delivery system.

A drug’s delivery system is defined by both the dosage form and the route of entry. Conventional drug delivery systems include oral, buccal, rectal, and intravenous systems. Within each category, there are multiple drug formats. For example, drug formats that can be delivered orally include tablets, capsules, and syrups.

Conventional drug delivery systems are common because they are convenient to take or administer. However, each delivery system, such as the oral delivery system, has its disadvantages. While it is relatively straightforward for most patients to chew or swallow a tablet or capsule, this delivery method may not be the most effective to administer a drug due to the first pass effect. This occurs because the effective concentration of the drug may be greatly reduced before it reaches the systemic circulation. Oral drugs may also be impractical for patients who have conditions that cause difficulty in swallowing solids or liquids.

Conventional drug delivery systems may not be practical or effective for every patient population and condition, thus leading to the development of alternative drug delivery systems. These novel drug delivery systems (NDDSs) include a range of systems from dissolvable film strips to ocular inserts. Alternative drug delivery systems provide a safe and effective way to administer a controlled drug dose to the targeted location in the body.

In addition to potentially being beneficial to patients, NDDSs also present financial advantages to drug manufacturers and developers. The average cost and time required to develop a novel drug delivery system for an existing product is substantially less than the cost and time required to develop an entirely active pharmaceutical ingredient and formulation. Manufacturers or developers may develop an alternative delivery method for their top-selling product to extend the life cycle of the product or increase their market share. Manufacturers can also reformulate an existing product to make it better suited to a specific patient population such as the geriatric or pediatric population.

How Can Novel Drug Delivery Systems Improve Upon Conventional Delivery Systems?

There are many reasons a drug manufacturer might decide to formulate a product that uses a novel drug delivery system. Major benefits of NDDSs include:

Controlled Delivery. Manufacturers may develop new medications to deliver the optimum dose to the site of action at the right time. NDDSs often bypass first pass metabolism, which means there is no significant reduction in the amount of the drug before it enters the bloodstream.

Enhanced Solubility. Low solubility is a significant challenge for drug manufacturers. A manufacturer’s chemists may need to develop a new formulation to enhance the solubility of poorly soluble drugs. Enhancing a drug’s solubility will improve its ability to be processed by the patient’s body.

Improved Stability. A major challenge for drug manufacturers is developing a product that will maintain its potency the entire time the patient stores and uses it. Manufacturers must ensure that their product retains 90 percent or more of its potency at its expiration date, and in some cases, this may mean developing a new, long-lasting drug formulation.

No Fluctuation of Drug Levels. With most conventional delivery systems, the drug is released immediately, and its levels may fluctuate in the bloodstream depending on the dosage form. NDDSs can be developed to keep a drug’s concentration in the therapeutically effective range.

Easier and Safer for Patients. Certain conventional drug delivery systems may be impractical or even unsafe for specific patient populations. Young children or adults with dysphagia might not be able to swallow a large capsule, for example. Manufacturers may need to develop NDDSs to ensure that the target patient population can take or receive the medication safely.

Reduction of Side Effects. By delivering the drug directly to its site of action, NDDSs can help minimize unpleasant and potentially harmful side effects associated with certain drugs in conventional delivery formats. This can improve a patient’s comfort and quality of life.

Improved Compliance. NDDSs can help reduce dosing frequency, make dose administration simpler, and eliminate the discomfort or unpleasantness associated with certain dosage formats (for example, a syrup with a bad taste), all of which can help improve patients’ medication compliance.

Efficient Use of APIs and Excipients. Reduced production costs can be an incentive for drug manufacturers to develop a unique formulation. NDDSs may help manufacturers use APIs and excipients more efficiently, leading to less waste and lower production costs.

Modes of Novel Drug Delivery Systems

There are three modes of NDDS that manufacturers should consider when planning a new drug formulation:

Targeted Drug Delivery System

A targeted drug delivery system transports medication to its site of action and avoids non-target organs, tissues, and cells. This allows a greater concentration of medication to be delivered to the target site and reduces the risk of side effects. Effective pharmaceutical carriers for targeted drug delivery systems include:

  • Lipoproteins
  • Liposomes
  • Micelles
  • Microcapsules
  • Microparticles
  • Nanoparticles
  • Polymers

Controlled Drug Delivery System

In a controlled drug delivery system, the drug’s formulation is modified for greater control of the release rate and exposure. This helps prolong the drug’s therapeutic effect and reduces fluctuation in the level of medication in the patient’s system. Pharmaceutical carriers for controlled drug delivery systems include:

  • Liposomes
  • Microspheres
  • Niosomes
  • Peptides
  • Polymeric Micelles
  • Proteins

Modulated Drug Delivery System

Modulated drug delivery systems rely on a medical device, such as a nebulizer or metered dose inhaler, to control and modulate the drug’s rate of release. Innovative approaches include magnetic, osmotic pressure-activated, and hydration-activated drug delivery systems.

NDDS In Action: Developing Dissolvable Oral Film Strips

Recent developments in oral films illustrate the many pathways available to drug manufacturers who are interested in formulating NDDS. Oral films are thin polymeric strips that can be designed to act either locally or systemically. They can be single or multi-layered, mucoadhesive or non-mucoadhesive, and designed for buccal, sublingual, palatal, or gastrointestinal absorption.

Until recently, oral films were only used for water soluble drugs because of their size and thickness. However, recent particle engineering techniques have made it possible to incorporate poorly soluble drugs into oral films, leading to new opportunities for manufacturers to develop fast-dissolving film strips.

There are many potential benefits of oral films over conventional drug delivery systems. Oral films provide:

  • Greater dosing accuracy than some other oral formats, such as solutions
  • Fast disintegration, dissolution, and action
  • Ease of administration (no need for water, chewing, or swallowing)
  • Portability and ease of handling

Developing an oral film can be a good option for manufacturers with patent-expiring drugs. Reformulating a current drug product as an oral film application will result in a three-year market exclusivity period due to the format’s novelty. Manufacturers will also potentially benefit by releasing a drug product that can be prescribed to previously unreached patient populations.

Challenges of Developing a Novel Drug Delivery System

While NDDSs present many exciting opportunities to drug manufacturers, they also come with a unique set of challenges.

Developing New Testing Methods. Testing methods used for other drug formulations are not always appropriate for NDDSs. For example, the type of disintegration and dissolution test used for capsules and tablets could not be used to evaluate a dissolving oral film strip. In many cases, NDDSs require the development and validation of new testing methods.

Evaluating Changes in Therapeutic Effect. Altering an existing drug’s delivery method may affect its rate of release, which can in turn affect the therapeutic response. Additional testing is required to determine how changing a drug’s delivery system changes the way it affects patients.

Improving Stability. A drug’s delivery method can also affect its stability. For example, micelles used as drug delivery carriers can have limited stability. Formulation scientists must explore ways to enhance the stability and longevity of a drug when altering its delivery system.

Scaling Up Production. After formulating a NDDS, manufacturers must ensure their production process is reproducible and consistent as they scale. Manufacturers will also have to evaluate the costs associated with large-scale production. In some cases, reformulating a drug may lead to lower production costs, but in others, the high cost of materials and the preparation method may make the NDDS difficult to scale.

Manufacturers must work with experienced formulation scientists to overcome the challenges of developing NDDS and reap the benefits of their many market opportunities.

Determining the Optimal Formulation for Your Drug

There is no single NDDS that will serve the needs of all drug manufacturers and patient populations. It is up to manufacturers and their formulation scientists to identify optimal NDDS by weighing a wide range of factors, including:

  • The physicochemical properties of the drug
  • Stability
  • Bioavailability
  • Site of action
  • Target population
  • Frequency of dosing
  • Target drug concentration
  • Biological barriers

Manufacturers who need help developing a novel drug delivery system, either for a new drug or existing product, should contact Avomeen for a consultation. Our team includes expert scientists and technical staff members who have spent years working with pharmaceutical companies. Our scientists have helped clients develop a diverse selection of NDDSs, including emulsions, microspheres, implants, and oral films. Avomeen can help your company identify and create a novel drug delivery system that garners you market exclusivity and improves your patients’ experience.

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