RESUMEN
Oral cancer is one of the most prevalent types of cancer head and neck cancers worldwide. Photodynamic therapy (PDT) has demonstrated great potential against cancers, reducing long-term morbidity. In this study, we investigated the incorporation of methylene blue (MB) in a mucoadhesive liquid crystal precursor system (LCPS) for oral cancer treatment. The photostability and the in vitro release, permeation, and retention profile of MB-loaded LCPS (MB-LCPS) were investigated, as well as its in vitro PDT activity against normal (HaCaT) and tumoral (HSC-3) cell lines. LCPS increased the photostability of MB and exhibited a prolonged release profile of MB. In addition, LCPS increased the retention of MB in the porcine esophageal mucosa by around 3 times higher than the MB solution. The retention of MB in LCPS was around 2 times greater than its permeability, which is suitable for guaranteeing the maintenance of the therapy in the oral cavity. In vitro cytotoxicity assay indicated that MB-LCPS increased the antitumoral activity of MB after 20 min of irradiation at 660 nm and 12.5 J/cm2. The results obtained suggest that the developed formulation is an interesting strategy for the potential application in the treatment of oral cancer by PDT.
Asunto(s)
Cristales Líquidos , Neoplasias de la Boca , Fotoquimioterapia , Animales , Porcinos , Fotoquimioterapia/métodos , Fármacos Fotosensibilizantes , Azul de Metileno , Neoplasias de la Boca/tratamiento farmacológicoRESUMEN
OBJECTIVE: To assess the efficacy of aerosolized midazolam, introduced through buccal versus intranasal mucosa in managing uncooperative children undergoing dental treatment. METHOD AND MATERIALS: A crossover randomized controlled clinical trial included 36 children aged 3 to 5 years, rated I or II according to the Frankl scale and ASA I or II. Each child fulfilled the requirement of having a dental condition that needed treatment in two dental settings. They were randomly assigned to one of two groups; either buccal or intranasal aerosolized midazolam was administered at the first visit. The alternate route was implemented with a 1-week washout period in the second visit. Drug acceptance and time until optimum sedation were measured. Crying, sleeping, head resistance, and child overall behavior were assessed using modified Houpt scale. RESULTS: In total, 34 patients (95 %) were drowsy on optimum sedation. There was a statistically higher acceptance of buccal midazolam (P < .001). Onset of optimum sedation was more rapid for the intranasal group, with a mean of 15.50 ± 4.226 minutes (P < .001), while in the buccal group the mean was 22.97 ± 4.582 minutes. No statistical differences were recorded between the two groups in all behavior rating scales, except for crying where the intranasal group was statistically higher (P = .010). Regarding the overall behavior, there was no significant difference recorded between the two groups (P = .204). CONCLUSION: Aerosolized buccal midazolam was more tolerated by the patients. However, intranasal aerosolized midazolam had a more rapid onset of sedation. Both buccal and intranasal administrations of aerosolized midazolam are safe and effective.
Asunto(s)
Anestesia Dental , Hipnóticos y Sedantes , Midazolam , Administración Intranasal , Preescolar , Sedación Consciente , Humanos , Hipnóticos y Sedantes/administración & dosificación , Midazolam/administración & dosificaciónRESUMEN
BACKGROUND: Buccal drug delivery is a fascinating research field. Gel-based formulations present potent characteristics as buccal systems since they have great physicochemical properties. METHODS: Among the various gels, in situ gels are viscous colloidal systems consisting of polymers; when physiological conditions change (pH, temperature, ion activation), they are transformed into the gel phase. These systems can improve bioavailability. Other systems, such as nanogels or emulgels can also be applied for buccal delivery with promising results. Polymeric gel-based systems can be produced by natural, semisynthetic, and synthetic polymers. Their main advantage is that the active molecules can be released in a sustained and controllable manner. Several gels based on chitosan are produced for the entrapment of drugs demonstrating efficient retention time and bioavailability due to chitosan mucoadhesion. Besides polysaccharides, poloxamers and carbopol are also used in buccal gels due to their high swelling ability and reversed thermal gelation behavior. RESULTS: Herein, the authors focused on the current development of mucoadhesive gel systems used in buccal drug delivery. After explaining buccal drug delivery and mucoadhesion, various studies with hydrogels, in situ gels, and nanogels were analyzed as buccal gel systems. Various mucoadhesive gel studies with mucoadhesive polymers have been studied and summarized. This review is presented as valuable guidance to scientists in formulating buccal mucoadhesive drug delivery systems. CONCLUSION: This review aimed to assist researchers working on buccal drug delivery by summarizing buccal drug delivery, mucoadhesion, and buccal mucoadhesive gel systems recently found in the literature.
Asunto(s)
Quitosano , Polímeros , Administración Bucal , Sistemas de Liberación de Medicamentos , Geles , Humanos , Hidrogeles , Mucosa Bucal , Poloxámero , ViscosidadRESUMEN
Considerable research exercises have been directed towards the development of efficient and safe drug delivery systems. Various materials are used in different pharmaceutical formulations for the development of efficient drug delivery systems in the treatment of disease. Biopolymers are a choice of research as an excipient delivery system due to their biodegradability, low toxicity, safe, stable, and renewable nature. Biopolymers are naturally occurring polymers or polymer matrix composites, that are extracted from animals, bacteria, fungi, and plants. Cellulose, starches are carbohydrate-based polymers, and wool, silk, gelatin, and collagen are protein-based biopolymers. Biopolymers are obtained from various sources but biopolymers, that belong to the carbohydrate origin, have been found very promising in drug delivery through various routes. The review mainly focuses on the biopolymers currently in use for buccal-mediated pharmaceutical drug delivery systems because the buccal route is an efficient drug delivery system that allows direct systemic circulation of drugs. It also prevents the hydrolysis of the drug molecule in the gastrointestinal tract and thus increases the bioavailability of the drug. The present review discusses the overview of other drug delivery routes, challenges with conventional drug delivery systems, pharmaceutical applications of some biopolymers used in buccal drug delivery systems, that are published recently, currently in use, or used over the past decade.
Asunto(s)
Sistemas de Liberación de Medicamentos , Preparaciones Farmacéuticas , Administración Bucal , Animales , Biopolímeros , PolímerosRESUMEN
Owing to the ease of the administration, the oral cavity is an attractive site for the delivery of drugs. The main difficulty for administration via the buccal route is an effective physiological removal mechanism of the oral cavity that takes way the formulation from the buccal site and decreases the bioavailability of drugs. The use of mucoadhesive polymers in buccal drug delivery shows assessing buccal drug permeation and absorption, however some studies bring an in vivo performance. This review points to the use of polymers in the manufacture of drug delivery systems (hydrogels, films and tablets) and shows the results of their in vivo performance tests.
Asunto(s)
Portadores de Fármacos/química , Preparaciones Farmacéuticas/metabolismo , Polímeros/química , Administración Bucal , Disponibilidad Biológica , Composición de Medicamentos , Humanos , Hidrogeles/química , Mucosa Bucal/metabolismo , Comprimidos/químicaRESUMEN
The buccal mucosa is accessible, shows rapid repair, has an excellent blood supply, and shows the absence of the first-pass effect, which makes it a very attractive drug delivery route. However, this route has limitations, mainly due to the continuous secretion of saliva (0.5 to 2 L/day), which may lead to dilution, possible ingestion, and unintentional removal of the active drug. Nanotechnology-based drug delivery systems, such as liquid crystalline systems (LCSs), can increase drug permeation through the mucosa and thereby improve drug delivery. This study aimed at developing and characterizing the mechanical, rheological, and mucoadhesive properties of four liquid crystalline precursor systems (LCPSs) composed of four different aqueous phases (i) water (FW), (ii) chitosan (FC), (iii) polyethyleneimine (FP), or (iv) both polymers (FPC); oleic acid was used as the oil phase, and ethoxylated and propoxylated cetyl alcohol was used as the surfactant. Polarized light microscopy and small-angle X-ray scattering indicated that all LCPSs formed liquid crystalline states after incorporation of saliva. Rheological, texture, and mucoadhesive assays showed that FPC had the most suitable characteristics for buccal application. In vitro release study showed that FPC could act as a controlled drug delivery system. Finally, based on in vitro cytotoxicity data, FPC is a safe buccal drug delivery system for the treatment of several buccal diseases.
Asunto(s)
Quitosano/química , Sistemas de Liberación de Medicamentos/métodos , Mucosa Bucal , Polietileneimina/química , Polímeros/química , Administración Bucal , Línea Celular Transformada , Quitosano/administración & dosificación , Humanos , Cristales Líquidos/química , Mucosa Bucal/efectos de los fármacos , Mucosa Bucal/metabolismo , Polietileneimina/administración & dosificación , Polímeros/administración & dosificación , Reología/métodos , Tensoactivos/administración & dosificación , Tensoactivos/químicaRESUMEN
Non-invasive insulin delivery systems have potential to overcome the most pressing problem regarding effective treatment of diabetic patients: therapy compliance. To overcome this disadvantage, non-invasive routes such as oral, buccal, pulmonary, nasal and transdermal have been proposed. These new routes of insulin administration may help to suppress hypoglycemia episodes and aid to control weight gain and post-meal glucose. Despite all efforts the invasive route remains preferential, since studies on insulin administration by non-invasive routes conducted to date have not demonstrated clinical efficacy and safety, including some products introduced in the market. Therefore, the aim of this review is to make an update of the current state of administration of insulin by non-invasive routes as alternatives to the conventional invasive route.