Buccal delivery system of active pharmaceutical ingredients-ionic liquid (API-IL): effects of API-IL loading and gelatin film concentration

Ionic liquid (IL) salt of active pharmaceutical ingredient (API) represents a promising formulation strategy to address low drug solubility and polymorphism prevalent in API solid crystals. The present work developed for the first time a buccal delivery system of API-IL via fast-dissolving API-IL-lo...

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Main Authors: Ng, Liu Han, Hadinoto, Kunn
Other Authors: School of Chemistry, Chemical Engineering and Biotechnology
Format: Article
Language:English
Published: 2024
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Online Access:https://hdl.handle.net/10356/173236
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Institution: Nanyang Technological University
Language: English
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spelling sg-ntu-dr.10356-1732362024-01-22T00:54:46Z Buccal delivery system of active pharmaceutical ingredients-ionic liquid (API-IL): effects of API-IL loading and gelatin film concentration Ng, Liu Han Hadinoto, Kunn School of Chemistry, Chemical Engineering and Biotechnology Engineering::Chemical engineering Drug Delivery System Poorly Soluble Drugs Ionic liquid (IL) salt of active pharmaceutical ingredient (API) represents a promising formulation strategy to address low drug solubility and polymorphism prevalent in API solid crystals. The present work developed for the first time a buccal delivery system of API-IL via fast-dissolving API-IL-loaded gelatin films. Imidazolium-based ibuprofen salt was used as the model API-IL. The effects of API-IL loading and gelatin concentration on the film's (i) mechanical strength, (ii) inter-batch uniformity in the films’ API payload, weight, and thickness, (iii) thermal stability, (iv) API dissolution and solubility enhancement were investigated. The plasticizer role of API-IL was evident, where minimum 30 wt% API-IL loading was needed to produce flexible yet mechanically-strong films. Lower API-IL loading produced brittle films due to insufficient plasticization facilitated by hydrogen bond interactions between API-IL and gelatin. Gelatin concentration influenced films’ mechanical strength, weight/thickness, and API dissolution rate. Depending on the API-IL loading and gelatin concentration, films with API payload (7–30 mg/cm2), thickness (300–900 µm), and weight (20–110 mg/cm2) were produced at nearly 100% efficiency and high inter-batch uniformity. API-IL existed as amorphous liquid in the film exhibiting fast API dissolution (100% in 15 min) and high kinetic solubility (8 times thermodynamic solubility) in simulated saliva fluid. Ministry of Education (MOE) The authors would like to thank Ministry of Education Singapore for the postgraduate scholarship awarded to L.H. Ng. 2024-01-22T00:54:46Z 2024-01-22T00:54:46Z 2024 Journal Article Ng, L. H. & Hadinoto, K. (2024). Buccal delivery system of active pharmaceutical ingredients-ionic liquid (API-IL): effects of API-IL loading and gelatin film concentration. Chemical Engineering Research and Design, 202, 115-125. https://dx.doi.org/10.1016/j.cherd.2023.12.027 0263-8762 https://hdl.handle.net/10356/173236 10.1016/j.cherd.2023.12.027 2-s2.0-85180532311 202 115 125 en Chemical Engineering Research and Design © 2023 Institution of Chemical Engineers. Published by Elsevier Ltd. All rights reserved.
institution Nanyang Technological University
building NTU Library
continent Asia
country Singapore
Singapore
content_provider NTU Library
collection DR-NTU
language English
topic Engineering::Chemical engineering
Drug Delivery System
Poorly Soluble Drugs
spellingShingle Engineering::Chemical engineering
Drug Delivery System
Poorly Soluble Drugs
Ng, Liu Han
Hadinoto, Kunn
Buccal delivery system of active pharmaceutical ingredients-ionic liquid (API-IL): effects of API-IL loading and gelatin film concentration
description Ionic liquid (IL) salt of active pharmaceutical ingredient (API) represents a promising formulation strategy to address low drug solubility and polymorphism prevalent in API solid crystals. The present work developed for the first time a buccal delivery system of API-IL via fast-dissolving API-IL-loaded gelatin films. Imidazolium-based ibuprofen salt was used as the model API-IL. The effects of API-IL loading and gelatin concentration on the film's (i) mechanical strength, (ii) inter-batch uniformity in the films’ API payload, weight, and thickness, (iii) thermal stability, (iv) API dissolution and solubility enhancement were investigated. The plasticizer role of API-IL was evident, where minimum 30 wt% API-IL loading was needed to produce flexible yet mechanically-strong films. Lower API-IL loading produced brittle films due to insufficient plasticization facilitated by hydrogen bond interactions between API-IL and gelatin. Gelatin concentration influenced films’ mechanical strength, weight/thickness, and API dissolution rate. Depending on the API-IL loading and gelatin concentration, films with API payload (7–30 mg/cm2), thickness (300–900 µm), and weight (20–110 mg/cm2) were produced at nearly 100% efficiency and high inter-batch uniformity. API-IL existed as amorphous liquid in the film exhibiting fast API dissolution (100% in 15 min) and high kinetic solubility (8 times thermodynamic solubility) in simulated saliva fluid.
author2 School of Chemistry, Chemical Engineering and Biotechnology
author_facet School of Chemistry, Chemical Engineering and Biotechnology
Ng, Liu Han
Hadinoto, Kunn
format Article
author Ng, Liu Han
Hadinoto, Kunn
author_sort Ng, Liu Han
title Buccal delivery system of active pharmaceutical ingredients-ionic liquid (API-IL): effects of API-IL loading and gelatin film concentration
title_short Buccal delivery system of active pharmaceutical ingredients-ionic liquid (API-IL): effects of API-IL loading and gelatin film concentration
title_full Buccal delivery system of active pharmaceutical ingredients-ionic liquid (API-IL): effects of API-IL loading and gelatin film concentration
title_fullStr Buccal delivery system of active pharmaceutical ingredients-ionic liquid (API-IL): effects of API-IL loading and gelatin film concentration
title_full_unstemmed Buccal delivery system of active pharmaceutical ingredients-ionic liquid (API-IL): effects of API-IL loading and gelatin film concentration
title_sort buccal delivery system of active pharmaceutical ingredients-ionic liquid (api-il): effects of api-il loading and gelatin film concentration
publishDate 2024
url https://hdl.handle.net/10356/173236
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