Lysozyme is particularly attractive for the local treatment of oral pathologies related to microbiological infections. However, the requirement of a prolonged release is difficult to achieve because of saliva swallowing and of the protein denaturation which can occur during production and storage of a dosage form. This work demonstrates the feasibility to prepare lysozyme mucoadhesive tablets by freeze-drying. Tablets were prepared by using alginate (ALG) physically “cross-linked” with calcium ion and different grades of hydroxypropyl methylcellulose (HPMC) (i.e., E5, E50, or K100). The tablets were characterized in terms of swelling or erosion behavior, in vitro mucoadhesive properties, lysozyme activity (Micrococcus lysodeikticus), drug release and ability to inactivate Staphylococcus aureus. The formulations prepared with HPMC K100 were discarded because of the fast erosion. All other formulations allowed a sustained release over at least 6 h. Independently of composition, lysozyme activity (78,311 ± 1873 Units/mg) significantly decreased in the case of tablets containing 5% and 10% w/w of protein (55,000 Units/mg and 33,000 Units/mg, respectively). Conversely, no modifications occurred in the case of tablets containing 1% w/w lysozyme. The formulation prepared by ALG/HPMC E5 7/3 ratio was efficacious against S. aureus. After 3 months of storage at 5 ± 3°C, no significant decrease in lysozyme activity was observed.
Lysozyme Mucoadhesive Tablets Obtained by Freeze-Drying / C.G.M. Gennari, P. Sperandeo, A. Polissi, P. Minghetti, F. Cilurzo. - In: JOURNAL OF PHARMACEUTICAL SCIENCES. - ISSN 0022-3549. - 108:11(2019 Nov), pp. 3667-3674.
|Titolo:||Lysozyme Mucoadhesive Tablets Obtained by Freeze-Drying|
GENNARI, CHIARA GRAZIA MILENA (Primo) (Corresponding)
SPERANDEO, PAOLA (Secondo)
MINGHETTI, PAOLA (Penultimo)
CILURZO, FRANCESCO (Ultimo)
|Parole Chiave:||alginate; controlled release; dissolution; freeze drying; mucosal drug delivery; protein delivery|
|Settore Scientifico Disciplinare:||Settore CHIM/09 - Farmaceutico Tecnologico Applicativo|
|Data di pubblicazione:||nov-2019|
|Data ahead of print / Data di stampa:||22-ago-2019|
|Digital Object Identifier (DOI):||http://dx.doi.org/10.1016/j.xphs.2019.08.011|
|Appare nelle tipologie:||01 - Articolo su periodico|
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