Modulation of the clinically accessible gelation time using glucono-d-lactone and pyridoxal 5′-phosphate for long-acting alginate in situ forming gel injectable

The purpose of this study was to design alginate in situ forming gel (ISFG) injectable with clinically acceptable gelation time and controlled release of hydrophobic drug. Milled or unmilled paliperidone palmitate (PPP) was used. The gelation time was controlled by varying the ratios of glucono-d-lactone (GDL) and pyridoxal 5'-phosphate (PLP) in prefilled alginate solution mixtures (ASMs) containing PPP, CaCO3, GDL and PLP for clinically acceptable injectability. However, the gelation time was varied by the alginate type (M/G ratio), storage condition, and drug solubilizers. This ISFG exhibited 32.15 kPa of the maximal compressive stress without causing pain and stiffness. The ISFG containing conically milled PPP released PPP in a controlled manner without exhibiting any initial burst release for 4 weeks. The current alginate ISFG injectable using new combination of PLP and GDL could be used to deliver long-acting injectable drugs.

Automated summary

This study aimed to design an alginate in situ forming gel injectable with controlled release of hydrophobic drug and clinically acceptable gelation time. By adjusting the ratio of ingredients, the gelation time was controlled effectively to release the drug without initial burst release. This injectable has potential for delivering long-acting drugs.