Novel Colon-Specific Microspheres With Highly Dispersed Hydroxycamptothecin Cores: Their Preparation, ReleaseBehavior, and Therapeutic Efficiency Against Colonic Cancer

Development of a chemically stable 10-hydroxycamptothecin nanosuspensions

“…Due to the poor solubility of the lactone form, 10-HCPT is usually used in the more soluble form of carboxylate salt which is more toxic and less active. In order to develop high performance delivery systems for the insoluble lactone form 10-HCPT, pharmaceutical scientists have made a lot of efforts to develop, such as microspheres (Shenderova et al, 1997(Shenderova et al, , 1999Lu and Zhang, 2006), nanoparticles (Sun et al, 2004;Zhang et al, 2006aZhang et al, , 2007aGuo et al, 2007;Yang et al, 2007), niosomes (Shi et al, 2006;Hong et al, 2009), emulsions (Zhao et al, 2007), polymeric micelle systems (Zhang et al, 2007b) and prodrugs (He et al, 2004;Wang et al, 2005). However, these delivery systems also have some obvious limitations, such as low drug loading capacity, adverse effects induced by excipients or solvents, variability of effect and unpredictability of metabolism in vivo.…”

Preparation and pharmacodynamics of stearic acid and poly (lactic-co-glycolic acid) grafted chitosan oligosaccharide micelles for 10-hydroxycamptothecin

“…In order to develop high performance drug delivery systems for the insoluble lactone form of HCPT, many attempts have been made, such as polymer microshperes (Ertl et al, 1999;Shenderova et al, 1997;Shenderova et al, 1999;Lu and Zhang, 2006), liposomes Cortesi et al, 1997), emulsions (Cortesi et al, 1997;Zhao et al, 2007), nanoparticles (Sun et al, 2004;Zhang et al, 2006Zhang et al, , 2007aYang et al, 2007;Guo et al, 2007), niosomes (Shi et al, 2006;Hong et al, 2009) and prodrugs (Carbonero and Supko, 2002;O'Leary and Muggia, 1998;He et al, 2004;Wang et al, 2005). However, these delivery systems still have some obvious limitations, such as low drug loading capacity, adverse effects induced by excipients or sol- vents.…”

Preparation and Physicochemical Properties of 10-Hydroxycamptothecin (HCPT) Nanoparticles by Supercritical Antisolvent (SAS) Process

“…Therefore, it is of great significance in developing the high performance delivery systems for the insoluble lactone form 10-HCPT. Recently, some novel delivery systems of HCPT have been reported, such as nanosuspensions [5], prodrugs [6–9], nanoparticles [10,11], microspheres [12–14], niosomes [3], emulsions [15] and polymeric micelle systems [16,17]. Among these tested approaches, nanosuspensions system, a sub-micro colloidal dispersion system, is considered as one of the most promising methods because of its characteristics in drug loading, release, delivery, stability and various options for administration, such as oral, parenteral, ocular and pulmonary pathways [18].…”