The European Medicines Agency (EMA) and the Current Good Manufacturing Practices (cGMP) in the United States of America, define excipient as the constituents of the pharmaceutical form other than the active ingredient, i.e., any component that is intended to furnish pharmacological activity. Although dendrimers do not have a pharmacopoeia monograph and, therefore, cannot be recognized as a pharmaceutical excipient, these nanostructures have received enormous attention from researchers. Due to their unique properties, like the nanoscale uniform size, a high degree of branching, polyvalency, aqueous solubility, internal cavities, and biocompatibility, dendrimers are ideal as active excipients, enhancing the solubility of poorly water-soluble drugs. The fact that the dendrimer's properties are controllable during their synthesis render them promising agents for drug-delivery applications in several pharmaceutical formulations. Additionally, dendrimers can be used for reducing the drug toxicity and for the enhancement of the drug efficacy. This review aims to discuss the properties that turn dendrimers into pharmaceutical excipients and their potential applications in the pharmaceutical and biomedical fields.

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Dendrimers as Pharmaceutical Excipients: Synthesis, Properties, Toxicity and Biomedical Applications.

Intranasal delivery of systemic-acting drugs: Small-molecules and biomacromolecules

The aim of this study was to investigate the presence of a possible direct correlation between vesicle elasticity and the amount of drug reaching the brain intranasally. Therefore, transfersomes were developed using phosphatidylcholine (PC) as the lipid matrix and sodium deoxycholate (SDC), Span® 60, Cremophor® EL, Brij® 58, and Brij® 72 as surfactants. The influence of the type of surfactant and PC-to-surfactant ratio on vesicle morphology, size, membrane elasticity, drug entrapment, and in vitro drug release was studied. The prepared transfersomes were mainly spherical in shape, with diameters ranging from 310 to 885 nm. Transfersomes containing SDC and Span 60 with optimum lipid-to-surfactant molar ratio showed suitable diameters (410 and 380 nm, respectively) and deformability indices (17.68 and 20.76 mL/sec, respectively). Values for absolute drug bioavailability in rat plasma for transfersomes containing SDC and those containing Span 60 were 24.75 and 51.35%, whereas AUC0–360min values in rat brain ...

Brain delivery of olanzapine by intranasal administration of transfersomal vesicles.

Introduction: In recent years, the wider use of nanotechnology has attracted greater attention from scientists in multi-disciplinary fields. Nanotechnological research has come a long way i...

https://www.tandfonline.com/doi/pdf/10.1080/1061186X.2017.1367006

General overview of lipid-polymer hybrid nanoparticles, dendrimers, micelles, liposomes, spongosomes and cubosomes.

Transdermal absorption enhancement of papain loaded in elastic niosomes incorporated in gel for scar treatment

This review gives concise information about the dendrimers, properties, synthesis and application in drug delivery, diagnosis and therapy. Due to their unique architecture these have improved physical and chemical properties. They show high solubility, miscibility and reactivity due to their terminal groups. Dendrimers have well defined size, shape, molecular weight and monodispersity. These properties make the dendrimers a suitable carrier in drug delivery application. Dendrimers are unimolecular miceller in nature and due to this enhances the solubility of poorly soluble drugs. Their compatibility with DNA, heparin and polyanions make them more versatile. Dendrimers, also referred as modern day polymers, they offer much more good properties than the conventional polymers. Due to their multivalent and mono disperse character dendrimers have stimulated wide interest in the field of chemistry biology, especially in applications like drug delivery, gene therapy and chemotherapy. Self assembly produces a faster means of generating nanoscopic functional and structural systems. But their actual utility in drug delivery can be assessed only after deep understanding of factors affecting their properties and their behavior in vivo. Key words : Dendrimers, PAMAM, monodispersity, Divergent-Convergent synthesis, carrier for drug delivery

/pdf/dendrimers-in-drug-delivery-diagnosis-and-therapy-basics-and-ufrxd5mazu.pdf

Dendrimers in drug delivery, diagnosis and therapy: basics and potential applications

This review gives concise information about the application of dendrimers in the field of drug delivery. Due to their unique architecture these have improved physical and chemical properties. Due to their terminal groups these show high solubility, miscibility and reactivity. Dendrimers have well defined size, shape, molecular weight and monodispersity. These properties make the dendrimers a suitable carrier in drug delivery application. Dendrimers are unimolecular miceller in nature and due to this enhances the solubility of poorly soluble drugs. Their compatibility with DNA, heparin and polyanions make them more versatile. Dendrimers, also referred as modern day polymers, they offer much more good properties than the conventional polymers. Due to their multivalent and mono disperse character dendrimers have stimulated wide interest in the field of chemistry biology, especially in applications like drug delivery, gene therapy and chemotherapy. Self assembly produces a faster means of generating nanoscopic functional and structural systems. But their actual utility in drug delivery can be assessed only after deep understanding of factors affecting their properties and their behavior in vivo . Key words: Dendrimers, Drug targeting, nanoscale carriers.

/pdf/potential-application-of-dendrimers-in-drug-delivery-a-3f8upgepz8.pdf

Potential application of dendrimers in drug delivery: a concise review and update

The aim of the present study was to investigate the potential of transfersomal formulations for transdermal delivery of indinavir sulfate and to evaluate Span 80, Tween 80, Sodium cholate and Sodium deoxycholate as edge activators. Vesicles containing phosphatidylcholine (PC) mixed with edge activators and indinavir sulfate were prepared by conventional rotary evaporation method and characterized for various parameters including vesicles shape and surface morphology, size and size distribution, entrapment efficiency, elasticity, turbidity, and in vitro drug release. The compositions of refined formulations were predicted, liposomes prepared, and tested against control. Skin permeation profile of transfersomal formulation bearing indinavir sulfate was observed and the investigations revealed an enhanced transdermal flux (8.91±0.9 µg/cm2 /hr) and decrease lag time (0.9 hr) for indinavir sulfate. The obtained flux was nearly 7.5 and 12.04 times higher than conventional liposomal formulation bearing indinavir sulfate and plain drug solution. These results suggested that transfersomes are potential vehicles for improved transdermal delivery of indinavir sulfate and Span 80, Tween 80 and Sodium cholate were equivalent to Sodium deoxycholate as edge-activators.

Enhanced Transdermal Delivery of Indinavir Sulfate Via Transfersomes

Transmucosal nasal delivery is a promising drug delivery option where common drug administrations (e.g., intravenous, intramuscular, or oral) are inapplicable. Recently, it has been shown that many drugs have better bioavailability by nasal route than by oral route. This has been attributed to rich vasculature and a highly permeable structure of the nasal mucosa coupled with avoidance of hepatic first-pass elimination, gut wall metabolism and/or destruction in the gastrointestinal tract. The physiology of the nose presents obstacles, but offers a promising route for non-invasive systemic delivery of numerous therapies and debatably drug delivery route to the brain. To overcoming problems in nasal drug delivery requires deep understanding of the various factors affecting nasal delivery. Thus present review focuses on various aspects of nasal drug delivery with special emphasis to factors affecting nasal drug administration. Keywords: Transmucosal nasal delivery, hepatic first-pass metabolism, non-invasive, microemulsions, microspheres.

https://www.arjournals.org/index.php/ijdd/article/download/214/207

A review on factors affecting the design of nasal drug delivery system

The present work was envisaged to reduce the dosing frequency and improve patient compliance by designing and evaluating Sustained Release Mucoadhesive (SRM) microspheres of Metformin hydrochloride (MH) for effective control of diabetes type-2. Microspheres were prepared by emulsification solvent evaporation method using Sodium carboxy methyl cellulose (SCMC), Carbopol 934P (CP), and Hydroxyl propyl methyl cellulose K4M (HPMC) as a mucoadhesive polymers. Microspheres prepared were found discrete, spherical and free flowing. The microspheres exhibits good mucoadhesive properties and showed high drug entrapment efficiency. MH release from these microspheres was slow and extended and dependent on the type of polymer used. The mean particle size decreased and the drug release rate increased at higher Stirring speed of emulsion content. Among all the formulation, formulation F1 containing SCMC and F2 containing CP showed the best reproducible results and mucoadhesive profile with good surface morphology. The data obtained thus suggest that mucoadhesive microspheres can successfully design for sustained delivery of MH and to improve patient compliance.

https://papers.ssrn.com/sol3/Delivery.cfm/SSRN_ID3774725_code4562211.pdf?abstractid=3774725&mirid=1

Vijay Kumar Tilak

Papers

Dendrimers in drug delivery, diagnosis and therapy: basics and potential applications

Potential application of dendrimers in drug delivery: a concise review and update

Enhanced Transdermal Delivery of Indinavir Sulfate Via Transfersomes

A review on factors affecting the design of nasal drug delivery system

Design and Evaluation of SRM Microspheres of Metformin Hydrochloride