Multilayered polymer coating modulates mucoadhesive and biological properties of camptothecin-loaded lipid nanocapsules

• Published in: International journal of pharmaceutics Vol. 635; p. 122792
• Main Authors: Isadora Boni, Fernanda, Noronha Ferreira, Natália, Fernanda Rodero, Camila, Franciane Leão, Aline, Stringhetti Ferreira Cury, Beatriz, Palmira Daflon Gremião, Maria
• Format: Journal Article
• Language: English
• Published: Netherlands Elsevier B.V 25.03.2023
• Subjects: Antiangiogenic activity; Camptothecin - chemistry; Camptothecin - pharmacology; Chitosan - chemistry; Chitosan lipid-core nanocapsule; Ex vivo permeation; Hyaluronic acid; Hypromellose phthalate; Lipids - chemistry; Nanocapsules - chemistry; Polymers - chemistry; Ex vivo permeation; Hyaluronic acid; Hypromellose phthalate; Chitosan lipid-core nanocapsule; Antiangiogenic activity
• ISSN: 0378-5173; 1873-3476
• DOI: 10.1016/j.ijpharm.2023.122792

[Display omitted] •High CPT loading in the nanocapsules was achieved.•Polymer coating provided mucoadhesiveness to nanocapsules.•Polymer coating modulated CPT intestinal permeation.•Nanoencapsulation preserved antiangiogenic activity of CPT. Lipid core nanocapsules (NCs) coated with multiple polymer layers were rationally designed as a potential approach for the colonic delivery of camptothecin (CPT). Chitosan (CS), hyaluronic acid (HA) and hypromellose phthalate (HP) were selected as coating materials, to modulate the mucoadhesive and permeability properties of CPT regarding the improvement of local and targeted action in the colon cancer cells. NCs were prepared by emulsification/solvent evaporation method and coated with multiple polymer layers by polyelectrolyte complexation technique. NCs exhibited spherical shape, negative zeta potential, and size ranged from 184 to 252 nm. The high efficiency of CPT incorporation (>94%) was evidenced. The ex vivo permeation assay showed that nanoencapsulation reduced the permeation rate of CPT through the intestinal mucosa by up to 3.5 times, and coating with HA and HP reduced the permeation percentage by 2 times when compared to NCs coated only with CS. The mucoadhesive capacity of NCs was demonstrated in gastric and enteric pH. Nanoencapsulation did not reduce the antiangiogenic activity of CPT and, additionally, it was observed that nanoencapsulation resulted in localized antiangiogenic action of CPT.