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Open AccessArticle

Combined Approach of Cyclodextrin Complexationand Nanostructured Lipid Carriers for the Development of a Pediatric Liquid Oral Dosage Form of Hydrochlorothiazide

1
Department of Chemistry, School of Human Health Sciences, University of Florence, Via Schiff 6, Sesto Fiorentino 50019 Florence, Italy
2
Department of Neuroscience, Psychology, Drug Research and Child Health (NEUROFARBA), Pharmacology and Toxicology Section, University of Florence, Viale Pieraccini 6, 50139 Florence, Italy
*
Author to whom correspondence should be addressed.
Pharmaceutics 2018, 10(4), 287; https://doi.org/10.3390/pharmaceutics10040287
Received: 26 November 2018 / Accepted: 17 December 2018 / Published: 19 December 2018
(This article belongs to the Special Issue Cyclodextrins in Drug Formulation and Delivery)
The development of specific and age-appropriate pediatric formulations is essential to assure that all children and their care-givers can easily access to safe and effective dosage forms. The need for developing specific pediatric medicinal products has been highlighted by the European Medicines Agency. The aim of this study was to investigate the effectiveness of combining the advantages of both cyclodextrin (CD) complexation and loading into nanostructured lipid carriers (NLC), to obtain a liquid oral pediatric formulation of hydrochlorothiazide (HCT), endowed with safety, dosage accuracy, good stability and therapeutic efficacy. Equimolar drug combinations as physical mixture (P.M.) or coground product (GR) with hydroxypropyl-β-cyclodextrin (HPβCD) or sulfobutylether-β-cyclodextrin (SBEβCD) were loaded into NLC, then characterized for particle size, homogeneity, Zeta potential, entrapment efficiency, gastric and storage stability. The presence of HPβCD allowed higher entrapment efficacy than NLC loaded with the plain drug, and enabled, in the case of GR systems a complete and sustained drug release, attributable to the wetting and solubilising properties of HPβCD toward HCT. In vivo studies on rats proved the superior therapeutic effectiveness of HCT-in HPβCD-in NLC formulations compared to the corresponding free HCT-loaded NLC, thus confirming the successfulness of the proposed approach in the development of an efficacious liquid oral formulation of the drug. View Full-Text
Keywords: hydrochlorothiazide; drug-in cyclodextrin-in nanostructured lipid carriers; oral liquid formulations for children; gastric stability; storage stability; in vivo diuretic effect hydrochlorothiazide; drug-in cyclodextrin-in nanostructured lipid carriers; oral liquid formulations for children; gastric stability; storage stability; in vivo diuretic effect
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MDPI and ACS Style

Cirri, M.; Maestrelli, F.; Mura, P.; Ghelardini, C.; Di Cesare Mannelli, L. Combined Approach of Cyclodextrin Complexationand Nanostructured Lipid Carriers for the Development of a Pediatric Liquid Oral Dosage Form of Hydrochlorothiazide. Pharmaceutics 2018, 10, 287.

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