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Novel Formulation Approaches
Besides standard formulation development, we provide services involving novel formulation approaches.
The liposome is one of the novel formulation approaches as a carrier of therapeutic molecules such as peptides. They are considered to be non-toxic, biodegradable and non-immunogenic, and have been used on several commercial pharmaceutical products. Liposomes serve as a reservoir for the drug, thus change the pharmacokinetics of the drug and significantly decrease its unwanted properties such as toxicity or serious side effects. Also the drug is prevented from early degradation or inactivation after introduced into the human body.
Creative Peptides is experienced in formulation development utilizing liposome-based on the properties of your APIs. This technology can be used on both hydrophilic and hydrophobic peptides.
Micelles and Reverse Micelles
Micelles can be used as a delivery system for peptide drugs. It has been shown that they can increase drug solubility, circulation time, reduce toxicity and enhance tissue penetration and specificity.
There are different types of micelles. Regular micelles (Figure A) are self-assemblies of amphiphilic copolymers in an aqueous medium. It can be used as formulation method for drugs that have poor solubility. Reverse micelles (Figure B) are self-assemblies of amphiphilic copolymers in a nonaqueous medium, and they can be used for the delivery of hydrophilic drugs.
Peptide drug-polymer conjugates are an advanced way to sustain drug release from Micelles. The micelles are formed from a conjugate of the drug with the hydrophobic part of an amphiphilic polymer.
Our team is specialized in developing micelles for peptide therapeutics.
An emulsion is a mixture of two or more liquids in which one is dispersed in the other as microscopic or ultramicroscopic droplets. Emulsion protects drug from degradation caused by acid and proteases in the GI tract, and it can enhance permeation of the drug through intestinal mucosa, which is beneficial for peptide-based APIs.
Chemical modification of peptide-based APIs can potentially improve their resistance against enzymatic degradation and/or membrane penetration. It can also be used to decrease immunogenicity.
Increasing the hydrophobicity of a drug by modification using hydrophobic group may increase its transcellular absorption, and it has been used on peptide-based drugs such as insulin.
Our team has the specialties to design chemical modifications based on the structure of your APIs in formulation development studies.
 Kozubek A et al, Liposomal drug delivery, a novel approach: PLARosomes. Acta Biochim Pol. 2000;47(3):639-49.
 Trivedi R et al, Nanomicellar formulations for sustained drug delivery: strategies and underlying principles Nanomedicine (Lond). 2010 Apr;5(3):485-505.
 Shaji J et al, Protein and Peptide Drug Delivery: Oral Approaches. Indian J Pharm Sci. 2008 May-Jun;70(3):269-77.
 Gupta S et al, Oral delivery of therapeutic proteins and peptides: a review on recent developments. Drug Deliv. 2013 Aug;20(6):237-46.