Jetting manufacturing of resins for solid-phase peptide synthesis

corresponding

Othman Al Musaimi1,2, Simona Serban3, Yahya E. Jad1,2, Zhichao Ma3, Ashish Kumar1,2, Cheng Ji3, Beatriz G. De La Torre2, Alessandra Basso3*, Fernando Albericio1,4*

*Corresponding authors
1. Peptide Science Laboratory, School of Chemistry and Physics, University of KwaZulu-Natal, Durban, South Africa
2. KwaZulu-Natal Research Innovation and Sequencing Platform (KRISP), School of Laboratory Medicine and Medical Sciences,
College of Health Sciences, University of KwaZulu-Natal, Durban, South Africa
3. Purolite, Llantrisant, United Kingdom
4. CIBER-BBN, Networking Centre on Bioengineering, Biomaterials and Nanomedicine and Department of Organic Chemistry,
University of Barcelona, Barcelona, Spain

Abstract

Peptides are an important class of Active Pharmaceutical Ingredients. Indeed, it is now feasible to synthesize peptides of up to forty amino acids in a multi-kilogram scale. This achievement has been made thanks to the implementation of the solid-phase synthesis methodology described by the Nobel Laureate R. Bruce Merrifield in 1963. Successful solid-phase peptide synthesis depends directly on the quality of the polymeric support, namely the resin. Here we describe new polystyrene in-house resins produced by ‘Jetting’ technology. The excellent properties (swelling, loading, particle size distribution, morphological structure) of these resins assure the quality of the final peptide.


INTRODUCTION

The pharmaceutical business is unique in the industrial arena as it is completely transdisciplinary. The process of taking an idea to the market requires the efforts of hundreds if not thousands of professionals from numerous disciplines. Importantly, even the customers (patients) play a key role in the clinical trials during the drug development phase.
It takes between 10 and 15 years for a new drug to reach the market, a period that far exceeds that required for products manufactured by other sectors. The investment required for getting a new drug onto the market is also a differential trait (US $1 billion). Together, all these factors make the pharmaceutical industry one of the most intriguing, and more so when you consider that at some point in our lives we will all become customers of this sector.

Briefly, Active Pharmaceutical Ingredients (APIs) can be divided into two groups, namely New Chemical Entities (NCEs) and Biologics, which can be differentiated by their production method. While NCEs are produced by chemical synthesis, the latter are manufactured using biotechnology. However, among NCEs there is a special class ...