Abstract
Objective: To develop and characterize Piper retrofractum extract loaded nanostructured lipid carriers (PRE loaded NLCs) for topical oral cavity administration to enhance bioavailability and stability of piperine.Methods: PRE loaded NLCs were prepared with a hot high-pressure homogenization technique followed by coating the particle surface with mucoadhesive polymers; polyethene glycol 400 (PEG) and polyvinyl alcohol (PVA). The physicochemical properties in terms of particle size, polydispersity index, zeta potential, drug entrapment efficiency, in vitro drug release profile and antimicrobial activities were examined. In vitro, mucoadhesion studies were assessed by the wash-off test. The physicochemical stabilities of mouth spray containing PRE loaded NLCs were investigated by kept at room temperature and 4 °C for 6 mo.Results: The PRE loaded NLCs showed spherical shape with a mean particle size of ~100-120 nm and zeta potential of ~-24 mV. Up to 90% drug entrapment efficiency was achieved. PEG-NLCs and PVA-NLCs showed a strong interaction with porcine buccal mucosa than uncoated-NLCs. All PRE loaded NLCs formulations revealed fast release characteristics and effective against Streptococcus mutans and S. sanguinis. The mouth spray containing PRE loaded NLCs showed good physical stability without particle aggregation. In addition, the chemical stability of piperine in NLCs was significantly improved during storage at both storage conditions compared to its solution form.Conclusion: The developed PRE loaded polymer coated-NLCs showed high potential to use as a local drug delivery system for reducing the bacterial growth in the oral cavity.
Highlights
Oral biofilm is a progressive and dynamic process of bacterial adhesion and colonization on the tooth and oral cavity surface
Dental caries and periodontitis are infectious diseases caused by oral pathogens that could be prevented by antibacterial agents
The ability of polyethene glycol 400 (PEG)-nanostructured lipid carriers (NLCs) and polyvinyl alcohol (PVA)-NLCs adhering on the mucosal surface improves the therapeutic efficiency of Piper retrofractum fruit extract (PRE) and/or other drugs by prolonging the residence time of the drug delivery system to the buccal mucosa tissue
Summary
Oral biofilm is a progressive and dynamic process of bacterial adhesion and colonization on the tooth and oral cavity surface. Several reports identify Streptococcus mutans and S. sanguinis as the main contributor in biofilm formation These bacteria adhere well to the tooth surface and produce a high amount of acid as well as extracellular polysaccharides (sticky glucan) resulting in demineralization of the enamel and further dental plaque formation that can lead to dental caries and periodontitis [1,2,3]. In order to maintain a sufficient therapeutic level, this formulation requires a frequent application which leads to poor patient compliance and increases local side effects due to the high concentration of the drug on the application site [9]. These limitations can be overcome with nanostructured lipid carriers (NLCs). NLCs improve therapeutic efficiency of the drug by prolonging the drug retention time on the buccal mucosa tissue [10], and by providing controlled drug release near the disease area
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