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Film Coatings Based on Aqueous Shellac Ammonium Salt “Swanlac® ASL 10” and Inulin for Colon Targeting

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Abstract

Over the past decades, increasing interests took place in the realm of drug delivery systems. Beyond treating intestinal diseases such as inflammatory bowel disease, colon targeting can provide possible applications for oral administration of proteins as well as vaccines due to the lower enzymatic activity in the distal part of GIT. To date, many strategies are employed to reach the colon. This article encompasses different biomaterials tested as film coatings and highlights appropriate formulations for colonic drug delivery. A comparison of different films was made to display the most interesting drug release profiles. These films contained ethylcellulose, as a thermoplastic polymer, blended with an aqueous shellac ammonium salt solution. Different blend ratios were selected as well for thin films as for coated mini-tablets, mainly varying as follows: (80:20); (75:25); (60:40). The impact of blend ratio and coating level was examined as well as the addition of natural polysaccharide “inulin” to target the colon. In vitro drug release was measured in 0.1 M HCl for 2 h followed by phosphate buffer saline pH 6.8 to simulate gastric and intestinal fluids, respectively. Coated mini-tablets were exposed to fresh fecal samples of humans in order to simulate roughly colonic content. Several formulations were able to fully protect theophylline as a model drug up to 8 h in the upper GIT, but allowing for prolonged release kinetics in the colon. These very interesting colonic release profiles were related to the amount of the natural polysaccharide added into the system.

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Data Availability

All data generated and/or analyzed during this study are included in this published article.

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Acknowledgements

The authors are deeply indebted to Prof. Pierre Desreumaux, Department of Gastroenterology CHU Lille, for the continuous support and advice. We would like to thank faithfully Mr. Rahul Mourya from A.F. Suter & Co Company in the UK for his generous supply of Shellac ASL 10 for film coatings. We are also deeply grateful to Dr. Tobias Hess from Chemische Fabrik Budenheim, in Germany, for his valuable supply of placebo mini-tablets.

Funding

M. Samuel Strich has received a salary from the university hospital of Lille (CHU: Centre Hospitalier Universitaire de Lille) to support his PhD within the framework of the hospital residency “IPR: Innovation Pharmaceutique et Recherche.” The authors are very grateful for this support. Sources of study funding have been from former industry research projects and University allocation of fund.

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Authors and Affiliations

  1. Univ. Lille, Inserm, CHU Lille, U1008, F-59000, Lille, France

    S. Strich, H. Azehaf, Y. Lellouche-Jacob, N. Medkour & Y. Karrout

  2. Univ. Lille, Inserm, CHU Lille, U1286_INFINITE, F-59000, Lille, France

    C. Neut

  3. PennConsult, Wormser Straße 28, 55276, Oppenheim, Germany

    M. Penning

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  1. S. Strich
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Contributions

S. Strich methodology; validation; investigation; visualization; conceptualization; writing—original draft—review and editing.

H. Azehaf review and editing; visualization

C. Neut methodology; validation; investigation; writing—review and editing.

Y. Lellouche-Jacob methodology; visualization; investigation.

N. Medkour methodology; visualization; investigation.

M. Penning methodology; validation; investigation; writing—review and editing

Y. Karrout conceptualization; methodology; resources; writing—original draft—review and editing; visualization; project administration; funding acquisition; supervision

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Correspondence to Y. Karrout.

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Strich, S., Azehaf, H., Neut, C. et al. Film Coatings Based on Aqueous Shellac Ammonium Salt “Swanlac® ASL 10” and Inulin for Colon Targeting. AAPS PharmSciTech 24, 205 (2023). https://doi.org/10.1208/s12249-023-02652-2

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