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Updated: Jan 31, 2026

Preparation of Neutrally-charged, pH-responsive Polymeric Nanoparticles for Cytosolic siRNA Delivery
Published on: May 2, 2019
Ion-pair approach coupled with nanoparticle formation to increase bioavailability of a low permeability charged drug
Isabel Lozoya-Agullo1, Marcos Planelles2, Matilde Merino-Sanjuán3
1Department of Pharmacokinetics and Pharmaceutical Technology, Miguel Hernandez University, San Juan de Alicante, 03550 Alicante, Spain; Department of Pharmacokinetics and Pharmaceutical Technology, University of Valencia, Av. de Blasco Ibáñez, 13, 46010 Valencia, Spain.
Abstract:
Atenolol is a drug widely used for the treatment of hypertension. However, the great drawback it presents is a low bioavailability after oral administration. To obtain formulations that allow to improve the bioavailability of this drug is a challenge for the pharmaceutical technology. The objective of this work was to increase the rate and extent of intestinal absorption of atenolol as model of a low permeability drug, developing a double technology strategy. To increase atenolol permeability an ion pair with brilliant blue was designed and the sustained release achieved through encapsulation in polymeric nanoparticles (NPs). The in vitro release studies showed a pH-dependent release from NPs, (particle size 437.30 ± 8.92) with a suitable release profile of drug (atenolol) and counter ion (brilliant blue) under intestinal conditions. Moreover, with the in vivo assays, a significant increase (2-fold) of atenolol bioavailability after administering the ion-pair NPs by oral route was observed. In conclusion, the combination of ion-pair plus polymeric NPs have proved to be a simple and very useful approach to achieve a controlled release and to increase the bioavailability of a low permeability charged drugs.
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