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Development of Novel Solid Nanostructured Lipid Carriers for Bioavailability Enhancement Using a Quality by Design Approach

  • Research Article
  • Advancements in Modified-release Oral Drug Delivery - Delivery throughout the Gastro-intestinal Tract
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Abstract

α, β-Arteether (ART) antimalarial drug is used to treat chloroquine-resistant malaria and cerebral malaria. The drug’s solubility in water is relatively low (17 μg/mL), and 40% of the drug degrades in the stomach, resulting in poor bioavailability. This article discusses the quality by design technique used for formulation development and optimization of nanostructured lipid carriers (NLCs). The ART-NLCs were made by solvent diffusion method. To develop solid NLCs, the NLCs were freeze-dried and encapsulated in enteric-coated capsule shells. The prepared NLCs showed particle size ranging between 156.8 ± 12 nm while zeta potential ranging between − 26.1 ± 0.22 mV. They also showed high encapsulation efficiency (> 85%) and an amorphous drug’s lipid matrix state. Pharmacokinetic parameters of optimized formulation enhance oral bioavailability to 18.45%. These investigations demonstrated the superiority of NLCs for improvement of solubility as well as oral bioavailability of poorly water-soluble drugs.

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Acknowledgements

The author, Ms. Neha Bajwa, thanks the Indian Council of Medical Research (ICMR), New Delhi, for funding her work as a senior research fellow under the ICMR-SRF scheme (F. No. 53/2019/-ECD-II dated 19/07/2019).

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Neha Bajwa prepared and formatted the research article and made a significant contribution to its inception and design, data collection, analysis, and interpretation. The creation of the tables and figures was assisted by Shipra Mahal and Shristi Naryal. The work was contextualized, organized, and evaluated by Preet Amol Singh. The project as well manuscript was supervised and evaluated by Dr. Ashish Baldi. The manuscript's published version has been read by all authors.

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Correspondence to Ashish Baldi.

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Bajwa, N., Mahal, S., Naryal, S. et al. Development of Novel Solid Nanostructured Lipid Carriers for Bioavailability Enhancement Using a Quality by Design Approach. AAPS PharmSciTech 23, 253 (2022). https://doi.org/10.1208/s12249-022-02386-7

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