Physicochemical evaluation of buccally administrated pilocarpine nanoparticles used against xerostomia

Hyposalivation (also referred to as xerostomia or dry mouth) causes a feeling of oral dryness and has an enormous impact on patients’ quality of life. Xerostomia treatment includes salivary substitutes and stimulants, the use of acids, and the administration of parasympathomimetic drugs, such as pilocarpine (PIL) [1] [2]. PIL in a naturally derived active pharmaceutical ingredient (API) that has extensive and pervasive effects on exocrine and smooth muscle tissues, by directly stimulating muscarinic receptors. Despite its clinical efficacy, the systematic administration of PIL (in the form of film-coated tablets) results in significant adverse events [3]. To overcome these side effects [4], local administration of the API in the buccal cavity is proposed. The aim of the present study was to evaluate the physicochemical properties of a new nanoparticulate (NP) formulation designed for the effective buccal administration of PIL.

Specifically, PIL-loaded NPs were fabricated using the double-emulsification process. Poly (lactic-co-glycolic acid) was used as a biodegradable matrix/carrier, while Carbopol-974P​ (CRB) as a coating and mucoadhesive agent. The physicochemical properties of the resulting NPs were evaluated by DSC, TGA, ATR-FTIR and pXRD. Results showed significant changes in the physicochemical properties of the NPs upon addition of the API and the coating agent (CRB). TGA showed that the prepared NPs were stable up to approximately 200°C, while pXRD diffractogram analysis revealed that, in all cases, the API was amorphously dispersed within the PLGA matrix/carrier. ATR-FTIR analysis confirmed the successful coating of CBR on the PIL-loaded PLGA NPs.

Funding This research has been co-financed by the European Regional Development Fund of the European Union and Greek national funds through the Operational Program Competitiveness, Entrepreneurship and Innovation, under the call RESEARCH – CREATE – INNOVATE (project code: T2EDK-00842).

 

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• References

• 1 Quilici D., Zech K.N.. Prevention and treatment options for medication-induced xerostomia. General dentistry 2019; 67 (04) 52-57
• 2 Turner M.D.. Hyposalivation and Xerostomia: Etiology, Complications, and Medical Management. Dental clinics of North America 2016; 60 (02) 435-43
• 3 Barbe A.G.. Medication-Induced Xerostomia and Hyposalivation in the Elderly: Culprits, Complications, and Management. Drugs & aging 2018; 35 (10) 877-885
• 4 Malallah O.S., Garcia C.M.A., Proctor G.B., Forbes B., Royall P.G.. Buccal drug delivery technologies for patient-centred treatment of radiation-induced xerostomia (dry mouth). International Journal of Pharmaceutics 2018; 541 (01) 157-16

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Artikel online veröffentlicht:
16. November 2023