Intranasal administration of budesonide-loaded nanocapsule microagglomerates as an innovative strategy for asthma treatment

Autor(es):Mostrar menos -

Ortiz, Manoel ; Coutinho, Diego de Sa ; Ciambarella, Bianca Torres ; de Souza, Everton Tenorio ; Leite D'Almeida, Ana Paula ; Durli, Tais Lusa ; Rodrigues e Silva, Patricia Machado ; Bernardi, Andressa ; Sonvico, Fabio ; Pohlmann, Adriana Raffin ; Martins, Marco Aurelio ; Guterres, Silvia Staniscuaski

• Tipo de documento: Artigo Científico
• Fonte: DRUG DELIVERY AND TRANSLATIONAL RESEARCH; v. 10, n. 6, p. 16-pg., 2020-08-12.

Resumo

The co-existence with rhinitis limits the control of asthma. Compared with oral H(1)receptor antagonists, intranasal corticosteroids have been demonstrated to provide greater relief of all symptoms of rhinitis and are recommended as first-line treatment for allergic rhinitis. Intrinsic limitations of nasal delivery, such as the presence of the protective mucous layer, the relentless mucociliary clearance, and the consequent reduced residence time of the formulation in the nasal cavity, limit budesonide efficacy to the treatment of local nasal symptoms. To overcome these limitations and to enable the treatment of asthma via nasal administration, we developed a budesonide-loaded lipid-core nanocapsule (BudNC) microagglomerate powder by spray-drying using a one-step innovative approach. BudNC was obtained, as a white powder, using L-leucine as adjuvant with 75 +/- 6% yield. The powder showed a bimodal size distribution curve by laser diffraction with a principal peak just above 3 mu m and a second one around 0.45 mu m and a drug content determined by HPLC of 8.7 mg of budesonide per gram. In vivo after nasal administration, BudNC showed an improved efficacy in terms of reduction of immune cell influx; production of eotaxin-1, the main inflammatory chemokine; and arrest of airways remodeling when compared with a commercial budesonide product in both short- and long-term asthma models. In addition, data showed that the results in the long-term asthma model were more compelling than the results obtained in the short-term model. (AU)

• Processo FAPESP: 14/50928-2 - INCT 2014: Nanotecnologia Farmacêutica: uma abordagem transdisciplinar
• Beneficiário: Maria Vitória Lopes Badra Bentley
• Modalidade de apoio: Auxílio à Pesquisa - Temático