Fast-Dissolving Nifedipine and Atorvastatin Calcium Electrospun Nanofibers as a Potential Buccal Delivery System.

Alhassan H. Aodah,Fatemah M. Alsulaihem,Ahmed J. Alfahad,Haitham A. Bukhary,Hassa A. Alshaya,Fahad A. Almughem,Salam Massadeh,Abdulrahman A. Halwani,Manal Alaamery,Ahmad M. Aldossary,Moutaz Y. Badr,Abdullah A. Alshehri,Essam A. Tawfik,Haya A. Alfassam

doi:10.3390/pharmaceutics14020358

Abstract

Geriatric patients are more likely to suffer from multiple chronic diseases that require using several drugs, which are commonly ingested. However, to enhance geriatric patients’ convenience, the electrospun nanofiber system was previously proven to be a successful alternative for the existing oral dosage forms, i.e., tablets and capsules. These nanofibers prepared either as single- or multi-layered fibers could hold at least one active compound in each layer. They might also be fabricated as ultra-disintegrated fibrous films for oral cavity administration, i.e., buccal or sublingual, to improve the bioavailability and intake of the administered drugs. Therefore, in this work, a combination of nifedipine and atorvastatin calcium, which are frequently prescribed for hypertension and hyperlipidemia patients, respectively, was prepared in a coaxial electrospinning system for buccal administration. Scanning electron microscopy image showed the successful preparation of smooth, non-beaded, and non-porous surfaces of the drug-loaded nanofibers with an average fiber diameter of 968 ± 198 nm. In contrast, transmission electron microscopy distinguished the inner and outer layers of those nanofibers. The disintegration of the drug-loaded nanofibers was ≤12 s, allowing the rapid release of nifedipine and atorvastatin calcium to 61% and 47%, respectively, after 10 min, while a complete drug release was achieved after 120 min. In vitro, a drug permeation study using Franz diffusion showed that the permeation of both drugs from the core–shell nanofibers was enhanced significantly (p < 0.05) compared to the drugs in a solution form. In conclusion, the development of drug-loaded nanofibers containing nifedipine and atorvastatin calcium can be a potential buccal delivery system.

Highlights

Geriatric patients aged 60 or older are more likely to suffer from multiple chronic diseases; they require more attention for their medicines [1]
The current study aims to fabricate nifedipine and atorvastatin calcium loaded in Polyvinylpyrrolidone (PVP) core–shell nanofibers as a potential buccal dosage form for two BCS class II drugs that are commonly used for geriatrics [20,21]
(36.5–38.0%), atorvastatin calcium was purchased from Sigma-Aldrich

Summary

Introduction

Geriatric patients aged 60 or older are more likely to suffer from multiple chronic diseases; they require more attention for their medicines [1]. According to WHO predictions, the number of people aged 60 years and over is expected to reach 1.4 billion by 2030 compared to only a billion in 2020. Several factors affect the nutritional status of older people, such as an insufficient chewing ability due to missing teeth or dentures, slow swallow reflex, difficulty in eating, a decrease in digestive enzymes, a decrease in minerals, vitamins, and drug absorption, and slow digestion rates [2]. Geriatric patients are expected to have poor compliance with the usual drug dosage forms, i.e., tablets and capsules [3,4]. New advanced techniques in pharmaceutical technology have emerged recently to overcome some of the obstacles and limitations of the conventional dosage forms such as the difficulty of swallowing the drugs, and have presented many oral dosage alternatives for geriatrics, such as buccal drug administration [3,5]

Methods

Results

Conclusion