Development of Oral Tablet Formulation Containing Erlotinib: Randomly Methylated-β-cyclodextrin Inclusion Complex...

Area of Science:

• Pharmaceutical Sciences
• Drug Delivery Systems
• Medicinal Chemistry

Background:

• Erlotinib (ERL) is a tyrosine kinase inhibitor used for metastatic non-small cell lung cancer (NSCLC).
• ERL exhibits low aqueous solubility, limiting its oral absorption and bioavailability.
• Complexation strategies can overcome these pharmacokinetic limitations.

Purpose of the Study:

• To develop and characterize an oral tablet formulation of ERL using randomly methylated-β-cyclodextrin (RAMEB-CD) inclusion complexes.
• To enhance the solubility and oral bioavailability of ERL for NSCLC treatment.

Main Methods:

• Erlotinib: RAMEB-CD inclusion complexes were prepared via co-lyophilization.
• Structural characterization utilized X-ray diffractometry and Fourier-transform infrared spectroscopy.
• Tablets were formulated using direct compression, and their physical properties (hardness, disintegration, dissolution) were evaluated.

Main Results:

• Co-lyophilization successfully formed stable ERL: RAMEB-CD inclusion complexes.
• Direct compression yielded tablets with acceptable physical characteristics and low moisture content.
• Dissolution studies demonstrated a significant increase in ERL solubility, with 99% drug release within 60 minutes.

Conclusions:

• The developed ERL: RAMEB-CD inclusion complex tablet formulation is a viable approach.
• This formulation enhances ERL dissolution and holds potential for improved oral bioavailability.
• It represents a promising alternative therapeutic strategy for NSCLC management.