Drug Formulation

Dose Forms

LSI  can move your APIs from pre-formulation, to the clinic, to commercial manufacturing, and will do it as cost-effectively, safely, and quickly as possible. We can handle many dose forms (see our article on the basics of dose forms:

  • tablets (fast release and controlled release)
  • capsules
  • enteric coatings
  • oral suspensions
  • oral control release films (buccal and sublingual patches)
  • topical creams and ointments
  • ocular (drops and ointments)
  • injectables (parenteral formulations)
  • liposomes
  • micro- and nano-encapsulation
  • proprietary drug delivery technologies (sol-gel encapsulation, smart hydrogels and biomaterials)
  • electrorheologically-controlled drug release
  • polyphosphazene polymers

Our services are supported by state-of-the-art analytical and bio-analytical laboratories, and our instrumentation includes HPLC, LC/MS, GC/MS, TGA/DSC, FT-IR, AA, particle size analysis, nanosizer, and other methods.

Injectables (Parenterals)

Preformulation Studies

Preformulation studies play a significant role in formulation development. Our scientists have decades of experience in determining the best route for formulating the target API or biotherapeutic. Our formulation strategy can be summarized as follows:

  • evaluating key physico-chemical characteristics of the target API
  • using physico-chemical data to develop a formulation strategy
  • determining the feasibility of implementing either a liquid or lyophilized parenteral formulation
  • developing screening tools to determine matrix effects (excipient compatibility with the drug)

Lyophilization

Lyophilization is critical for stabilizing drugs into stable dosage forms. These actives may undergo hydrolytic, oxidative, and aggregation reactions, compromising both potency and safety. In solution, some drugs are susceptible to degradation, and many proteins and antibodies may aggregate after repeated freeze/thaw cycles. Our lyophilization services overcome such issues by stabilizing these labile drugs and proteins. This means they are capable of:

  • facilitated global transport and storage
  • withstanding temperature changes
  • moving quickly through clinical trials

We can develop robust lyophilized formulations. Our formulation team is experienced in screening effective combinations of both aqueous and non-aqueous solvents, buffers, bulking agents, and lyo/cryo-protectants. We can determine critical formulation parameters that include:

  • collapse temperature (Tc)
  • eutectic melting temperature (Teu)
  • glass transition temperature
  • crystallization phenomena
  • the effects of annealing on ice crystal growth
  • solute structure

Formulation Development

After the preformulation work, we move on to formulation development, designing products to meet the performance criteria you set forth. We design our drug products not only to fit your product profile but also your clinical needs, because a well-formulated drug will avoid problems during clinical trials.

Our formulation expertise includes:

  • stabilizing the API through formulation and excipient selection
  • developing high- and low-concentration antibody or protein formulations
  • increasing the solubility and bioavailability of water-insoluble molecules
  • emulsions and liposomes (nanoparticles and microparticle delivery systems)
  • formulation development for early preclinical studies
  • process development for easy transition to large-scale production

Tablet Dose Forms

Preformulation Studies

Preformulation studies play a significant role in formulation development. Our scientists have decades of experience in determining the best route for formulating the target API into a solid dose form. Our formulation strategy is as follows:

  • initial assessment of the API’s physical state:
    • crystallinity/amorphous content
    • hygroscopicity
    • particle size, shape & surface area
    • moisture/solvent content
    • density (bulk and tap)
    • logP/LogD/pKa
    • solubility (physiological buffers)
    • enhanced solubility (solubility in co-solvents, surfactants, complexation agents, salts etc.)
    • solubility test for use in formulation and development of analytical methods for assessing stability
  • chemical and physical stability (heat, pH, light, humidity)
  • API-excipient compatibility (matrix effects)

During preformulation, we can rapidly characterize in detail the target API’s physico-chemical properties. These will be used in the early formulation stages to produce a stable and reproducible drug product.

Formulation Development

Using the information gleaned from the preformulation work, we develop a formulation strategy to meet your performance criteria and fit your desired product profile.

Our expertise includes:

  • formulating the API to fit your release profile: fast release, slow release, sublingual, etc.
  • increasing the solubility and bioavailability of water-insoluble molecules using excipients or micronization
  • matrix effects to ensure excipient and API compatibility
  • stability testing (accelerated and long-term)
  • enteric coatings
  • taste masking
  • formulation development for early preclinical trials and easy transition to large-scale production (detailed batch records and SOPs)

Contact us today to see how we can fill your formulation needs.