We report the synthesis and applications of a novel N-doped graphene quantum dots (GQDs) using hydrothermal reaction between citric acid and p-aminophenol. The synthesized N-doped GQDs have been characterized physico-chemically and evaluated its antioxidant, antimicrobial, DNA binding and cleavage activities. siRNA loading studies were performed and their effects on cells were evaluated. Obtained results indicate that monodisperse solution of N-doped GQDs has been obtained with particles size ca. ∼10.9 ± 1.3 nm. UV–Vis spectroscopy studies of the interactions between the N-doped GQDs and calf thymus DNA (CT-DNA) showed that the compound interact with CT-DNA via both intercalative and electrostatic binding. The DNA cleavage study showed that the N-doped GQDs cleaved DNA without any external agents. The antioxidant activity of N-doped GQDS was very active when compared to BHT. As the concentration of the compound increased, the antioxidant activity also increased. Cell viability assay demonstrated that the Ndoped GQDs showed cell viability (70%) when the concentration reached 200 μg/mL for A549 and also MDA-MB-231, 150 μg/mL for NIH-3T3 cell lines at 24 h incubation. N-doped GQDs were coated with Eudragit RS 100 and EphA2-siRNA was loaded. As a result of the studies on these formulations, it was concluded that there may be significant effects on A549 cells. The microscopy results revealed that N-doped GQDs was quickly internalized into the cell. Our novel N-doped-GQDs with siRNA are candidate for in situ tumor suppression via DNA and mRNA breakage.

Graphene quantum dots: Synthesis, characterization, cell viability, genotoxicity for biomedical applications

The rectal route is an effective route for the local and systemic delivery of active pharmaceutical ingredients. The environment of the rectum is relatively constant with low enzymatic activity and is favorable for drugs having poor oral absorption, extensive first-pass metabolism, gastric irritation, stability issues in the gastric environment, localized activity, and for drugs that cannot be administered by other routes. The present review addresses the rectal physiology, rectal diseases, and pharmaceutical factors influencing rectal delivery of drugs and discusses different rectal drug delivery systems including suppositories, suspensions, microspheres, nanoparticles, liposomes, tablets, and hydrogels. Clinical trials on various rectal drug delivery systems are presented in tabular form. Applications of different novel drug delivery carriers viz. nanoparticles, liposomes, solid lipid nanoparticles, microspheres, transferosomes, nano-niosomes, and nanomicelles have been discussed and demonstrated for their potential use in rectal administration. Various opportunities and challenges for rectal delivery including recent advancements and patented formulations for rectal drug delivery have also been included.

/pdf/advancements-in-rectal-drug-delivery-systems-clinical-trials-2fp4jcon.pdf

Advancements in Rectal Drug Delivery Systems: Clinical Trials, and Patents Perspective

In this work, the supercritical antisolvent (SAS) process was used to coprecipitate Eudragit L100-55 (EUD) with diclofenac (DICLO) and theophylline (THEOP), with the aim of obtaining composite microparticles with a prolonged drug release for oral delivery. Working at the optimized conditions in terms of pressure and overall concentration in the liquid solution (10.0 MPa and 50 mg/mL), microparticles of EUD/DICLO 20/1 and 10/1 w/w were produced with a mean size of 2.92 µm and 1.53 µm, respectively. For the system EUD/THEOP, well-defined spherical microspheres with a mean diameter ranging from 3.75 µm and 5.93 µm were produced at 12.0 MPa. The produced composite systems were characterized by various techniques, such as scanning electron microscopy, differential scanning calorimetry, X-ray microanalysis, FT-IR and UV-vis spectroscopy. Dissolution studies showed the potential of EUD to prolong the drug release, significantly, up to a few days.

https://www.mdpi.com/2073-4360/12/1/234/pdf

Eudragit: A Novel Carrier for Controlled Drug Delivery in Supercritical Antisolvent Coprecipitation.

Drugs with narrow absorption window (NAW) are those drugs that are absorbed from a specific region (most notably first part) of the gastrointestinal tract. Therefore, typical modified/sustained release formulations of those drugs cannot provide a true long-acting drug release. Once the dosage form has passed the absorption sites at the specific regions of the small intestine; the drug is no longer absorbed from the modified release dosage form and the bioavailability is adversely decreased. While there are many pharmacological classes such as centrally acting skeletal muscle relaxants, anti-parkinsonism drugs and anti-infective belong to NAW drugs and are required to be formulated in modified release dosage forms. Modified release dosage forms based on gastroretentive technologies could hold a promise. Such dosage forms aim to release drugs in the upper part of the gastrointestinal tract especially in the stomach in a controlled release manner that might provide sustained release characteristics without sacrificing much of total bioavailability. This review provides critical appraisal on different technologies, polymers, candidate drugs for gastroretentive technologies.

https://jabps.journals.ekb.eg/article_34068_70f660963c4829b85ff78237c6d20986.pdf

Gastro-retentive oral drug delivery systems: a promising approach for narrow absorption window drugs

Development of an effective vaccine is of paramount important in disease prevention and control. As such, recombinant technology can serve as a gateway for the development of safe and effective vaccines that can be delivered effectively with an appropriate adjuvant. Therefore, this paper aimed to review the role of recombinant vaccine technology, new adjuvants and the challenge of vaccine delivery. Related peer-reviewed journal article searches were conducted using a subscribed database at the Universiti Putra Malaysia library, involving areas of Health Sciences and Medicine via Medline, SCOPUS and Google Scholar. New generation vaccines include highly purified synthetic or recombinant antigens that stimulate effective cell-mediated immune and mucosal immunity. In order to enhance their efficacy, a number of adjuvants are used. Efforts have also been made to explore the usage of non-invasive routes of administration, devices and equipment for optimized antigen and immune-potentiator delivery of the immune system. Recombinant vaccine technology is rapid, compared to the traditional method of vaccine development and does not require the handling of live viruses. It is, therefore, a promising technology for developing a future vaccine to curb emerging and re-emerging viral infections that may be life-threatening or teratogenic.

An overview of recombinant vaccine technology, adjuvants and vaccine delivery methods

Polymers constitute the major part of pharmaceutical formulations functionality and significance. Development of novel drug delivery system (NDDS) has been made possible by eudragit polymers to modify the release pattern of drug. The basic objective of sustained drug release is to achieve more effective therapies by eliminating potential for both under and overdosing. Other advantages include maintenance of drug concentration with in desired range, fewer administration, optimal drug use and patient compliance. This review article gives outline of classification, nomenclature, physiological, and pharmaceutical properties of eudragit polymers. Eudragit polymers can be classified on the basis of use or type of formulation produced and includes time-controlled drug release by sustained release formulations, gastro-resistance and GI targeting by enteric formulations and moisture protection and odor/taste masking by protective formulations. Eudragit polymers are available in wide range of physical forms viz. aqueous dispersion, organic solution, granule and powder with varying degrees of solubility. Eudragit polymers have numerous drug release mechanism and wide applications in different drug delivery systems i.e. ophthalmic, buccal, sublingual, enteric, oral, colon, vaccine, gene, vaginal and transdermal drug delivery. It has been concluded that eudragit polymers have multifaceted applications in pharmacy and drug delivery system. Keywords: Eudragit, Time-controlled, Sublingual.

An overview of multifaceted significance of eudragit polymers in drug delivery systems

The aim of present study is to prepare microspheres of eudragit RL 100 loaded with Nefopam Hydrochloride by single emulsion solvent evaporation technique. Taguchi L9 orthogonal array design has been used to optimize the composition and operating conditions for preparation of formulations. Nine batches (F1-F9) were prepared by taking three independent variables (X 1 - drug: polymer ratio, X 2 - stirring speed and X 3 - stirring time) at three levels (+1, 0, -1). Response variables studied for batches (F1-F9) were mean particle size (µm) (Y 1 ), drug entrapment efficiency (% w/w) (Y 2 ) and drug loading (% w/w) (Y 3 ). Drug- polymer compatibility study was carried out by DSC and FTIR spectroscopy and indicates no physicochemical interaction. Microspheres were analyzed for morphological characteristics, mean particle size, drug entrapment efficiency, drug loading and in-vitro drug release. Percentage cumulative drug release for optimized batch F5 was found to be 85.421 ± 0.054 and followed higuchi model for release of drug.

/pdf/formulation-optimization-and-evaluation-of-sustained-release-29s4bhcjpi.pdf

Formulation, Optimization and Evaluation of Sustained Release Microspheres using Taguchi Design

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An overview of multifaceted significance of eudragit polymers in drug delivery systems

Formulation, Optimization and Evaluation of Sustained Release Microspheres using Taguchi Design