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The research aims to develop bionanosuspension using a biopolymer isolated from Fragaria ananassa fruit that constitutes potential and natural polymeric properties. At first, the biomaterial was isolated from the natural fruit pulp of Fragaria ananassa by an economical method of isolation. The model drug was nanosized by a novel sonication method. The isolated biopolymer was characterized for its polymeric properties, and its potential capabilities were evaluated in the delivery of nanosized phenytoin. The isolated biopolymer was characterized for DSC, FTIR, NMR, mass, and scanning electron microscopy. The isolated biomaterial was used for the preparation of phenytoin-loaded bionanosuspension with other excipients. The bionanoparticles were also characterized by different analytical testing such as FTIR, DSC, and SEM to confirm any interaction between model drug and biopolymer. The prepared bionanoparticles showed the release of phenytoin in a sustained manner over 36 hours. The release kinetic study was done using the BIT-SOFT 1.12 software and other parameters such as t50%, t80%, and r 2 were calculated. The formulation PFr6 was considered best having t50% in 18.22 hours and t80% in 29.62 h with an r2 value of 0.9793. This formulation showed up to 87.89% drug release within 36 hours. The prepared bio-nanosuspension was found to be stable and in a well-dispersed state. The dried bionanosuspension evaluation revealed no interaction between model drug and biopolymer without any loss of characteristic peaks. Therefore, the isolated biopolymer can be safely used to prepare stable bionanosuspension loaded with nanosized phenytoin.
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The article has been withdrawn at the request of the editor of the journal Current Drug Research Reviews due to incoherent content.Bentham Science apologizes to the readers of the journal for any inconvenience this may have caused.The Bentham Editorial Policy on Article Withdrawal can be found at https://benthamscience.com/editorial-policies-main.php BENTHAM SCIENCE DISCLAIMER: It is a condition of publication that manuscripts submitted to this journal have not been published and will not be simultaneously submitted or published elsewhere. Furthermore, any data, illustration, structure or table that has been published elsewhere must be reported, and copyright permission for reproduction must be obtained. Plagiarism is strictly forbidden, and by submit- ting the article for publication the authors agree that the publishers have the legal right to take appropriate action against the authors, if plagiarism or fabricated information is discovered. By submitting a manuscript, the authors agree that the copyright of their article is transferred to the publishers if and when the article is accepted for publication.
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Objective: Depression is one of the most frequent psychiatric and potentially life-threatening disorders. This research work can offer a potential for delivery of selegiline moiety via ocular route in bio-nanosuspension mode for the effective management of depression after preclinical performance screening. Methods: The selegiline-loaded bio-nanosuspension was prepared using novel bio-retardant isolated from fruit pulp of Manilkara zapota (Sapodilla) by sonication solvent evaporation method with different ratios (0.05%, 0.1%, 0.2%, 0.3%, 0.4%, 0.5%, and 1%) and with standard polymer HPMC (0.1%, 0.2%, 0.3%, 0.4%, and 0.5%). The prepared formulations were evaluated for pH stability studies, %entrapment efficiency, in vitro drug release, particle size, polydispersity index (PDI), zeta potential, and stability studies. Results: The prepared bio-nanosuspension was subjected to the best formulation based on comparison of above-mentioned evaluation parameters, so Fb2 (0.1%) formulation was found to be the best formulation showing an R2 value of 0.9814, T50% of 29.7 h, and T80% of 65.25 h. According to the release kinetics, the best fit model was found to be the Korsmeyer-Peppas with the Fickian diffusion (Higuchi matrix) as the mechanism of drug release. Manilkara zapota (Sapodilla) provided excellent stability for the formulation and resulting particle size for the best formulation was found to be 252 nm. The bio-nanosuspension had PDI of 0.35 with zeta potential of -8.91 mV. Conclusion: The prepared bio-nanosuspension was found to be safe and compatible with the ophthalmic delivery for treatment of depression.
Asunto(s)
Depresión/tratamiento farmacológico , Manilkara/química , Nanopartículas/química , Extractos Vegetales/química , Selegilina/administración & dosificación , Selegilina/química , Suspensiones/química , Química Farmacéutica/métodos , Sistemas de Liberación de Medicamentos , Liberación de Fármacos/efectos de los fármacos , Tamaño de la Partícula , Polímeros/química , Solubilidad/efectos de los fármacos , Solventes/química , Difracción de Rayos X/métodosRESUMEN
In this article a medicinal oil (neem oil) is fractionated and compared with original oil. The fractions were separated at low temperature using chloroform and methanol. The uniphase mixture of solvents and neem oil at room temperature was transformed to a bi-phasic system at low temperature. The isolated fractions (NOC - isolated using chloroform; NOM - isolated using methanol) were characterized and differentiated by GC, FT-IR and Rheometer. GC and FTIR have well revealed the difference in composition of fatty acids in fractions - NOC; NOM and neem oil (NO). Rheologically all the oils are different in viscosity from parent oil. The NOM fraction of neem oil showed newtonian behavior while NOC shows a non-newtonian behavior. It can be concluded from data that fractions NOC, NOM can be used for targeting drugs using various formulation approaches.
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Rapid developments in the field of molecular biology and gene technology resulted in generation of many macromolecular drugs including peptides, proteins, polysaccharides and nucleic acids in great number possessing superior pharmacological efficacy with site specificity and devoid of untoward and toxic effects. However, the main impediment for the oral delivery of these drugs as potential therapeutic agents is their extensive pre-systemic metabolism, instability in acidic environment resulting into inadequate and erratic oral absorption. Parenteral route of administration is the only established route that overcomes all these drawbacks associated with these orally less/inefficient drugs. But, these formulations are costly, have least patient compliance, require repeated administration, in addition to the other hazardous effects associated with this route. Over the last few decades pharmaceutical scientists throughout the world are trying to explore transdermal and transmucosal routes as an alternative to injections. Historically, oral transmucosal drug delivery has received intensive interest since ancient times for the most widely utilized route of administration for the systemic delivery of drugs. In more recent years, better systemic bioavailability of many drugs has been achieved by oromucosal route. Among the various transmucosal sites available, soft-palatal mucosa was also found to be the most convenient and easily accessible novel site for the delivery of therapeutic agents for systemic delivery as retentive dosage forms, because it has abundant vascularization and rapid cellular recovery time after exposure to stress. Smooth surface of the soft palate and its good flexibility are prerequisites to prevent mechanical irritation and local discomfort. The objective of this review is to provide an update on the most promising advances in novel non-invasive soft-palatal route and the conceptual and technical approaches to the design and formulation of soft-palatal drug delivery systems. In this area, the development of mucoadhesive delivery systems appears to be the most promising strategy.
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Sistemas de Liberación de Medicamentos/métodos , Mucosa Bucal/metabolismo , Hueso Paladar/metabolismo , Preparaciones Farmacéuticas/administración & dosificación , Administración a través de la Mucosa , Administración Oral , Animales , HumanosRESUMEN
The present study aimed to develop bilayered nail lacquer of terbinafine hydrochloride (TH) for treatment of onychomycosis. The composite nail lacquer formed an underlying drug-loaded hydrophilic layer and overlying hydrophobic vinyl layer. The hydrophilic lacquer made of hydroxylpropyl methylcellulose E-15 contained polyethylene glycol 400 (PEG 400) as a drug permeation enhancer. The vinyl lacquer was composed of poly (4-vinyl phenol) as a water-resistant film former. In vitro permeation studies in Franz diffusion cells indicated that the amount of TH permeated across the human cadaver nail in 6 days was 0.32 +/- 0.14, 1.12 +/- 0.42, and 1.42 +/- 0.53 microg/cm(2) from control (hydrophilic lacquer devoid of PEG 400), monolayer (hydrophilic lacquer alone), and bilayered nail lacquers, respectively. A higher nail drug load was seen in vitro with the bilayered lacquer (0.59 +/- 0.13 microg/mg) as compared to monolayer (0.36 +/- 0.09 microg/mg) and control (0.28 +/- 0.07 microg/mg) lacquers. The drug loss despite multiple washing was significantly low (p < 0.001) for the bilayered lacquer owing to the protective vinyl coating. Clinical studies demonstrated the efficacy of bilayered lacquer to achieve better drug load in the nail plate (1.27 +/- 0.184 microg/mg) compared to monolayer (0.67 +/- 0.18 microg/mg) and control (0.21 +/- 0.04 microg/mg) lacquers.
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Antifúngicos/uso terapéutico , Uñas , Naftalenos/uso terapéutico , Onicomicosis/tratamiento farmacológico , Antifúngicos/administración & dosificación , Antifúngicos/análisis , Cadáver , Rastreo Diferencial de Calorimetría , Cromatografía Líquida de Alta Presión , Femenino , Humanos , Masculino , Naftalenos/administración & dosificación , Naftalenos/análisis , TerbinafinaRESUMEN
Oral mucosal drug delivery is an alternative method of systemic drug delivery that offers several advantages over both injectable and enteral methods and also enhances drug bioavailability because the mucosal surfaces are usually rich in blood supply, providing the means for rapid drug transport to the systemic circulation and avoiding, in most cases, degradation by first-pass hepatic metabolism. The systems contact with the absorption surface resulting in a better absorption, and also prolong residence time at the site of application to permit once or twice daily dosing. For some drugs, this results in rapid onset of action via a more comfortable and convenient delivery route than the intravenous route. Not all drugs, however, can be administered through the oral mucosa because of the characteristics of the oral mucosa and the physicochemical properties of the drug. Although many drugs have been evaluated for oral transmucosal delivery, few are commercially available. The clinical need for oral transmucosal delivery of a drug must be high enough to offset the high costs associated with developing this type of product. Transmucosal products are a relatively new drug delivery strategy. Transmucosal drug delivery promises four times the absorption rate of skin. Drugs considered for oral transmucosal delivery are limited to existing products, and until there is a change in the selection and development process for new drugs, candidates for oral transmucosal delivery will be limited. The present papers intend to overview a wide range of orotransmucosal routes being potentially useful for transmucosal drug delivery and remind us of the success achieved with these systems and the latest advancement in the field.