Preparation and evaluation of a buflomedil hydrochloride niosomal patch for transdermal delivery.

CONTEXT: Niosomes are the non-ionic surfactant vesicles obtained on hydration of synthetic non-ionic surfactants. These are the promising vehicles for effective transdermal drug delivery. OBJECTIVE: The present research work was aimed to develop niosomal-based transdermal buflomedil hydrochloride patch containing a stable formulation with improved drug permeation. MATERIALS AND METHODS: Niosomes were prepared by solvent evaporation method using 32 factorial design. All the formulations were evaluated for vesicle size, zeta potential and percent entrapment efficiency. Optimized niosomal and liposomal formulation were loaded into a patch system. All the patches were then characterized for drug-excipient interaction study, scanning electron microscopy, pharmacotechnical properties and in vitro permeation studies. RESULT: F9 formulation having optimum vesicle size (10.09 ± 1.2 µm), highest zeta potential (-85.4 ± 0.56 mV) and maximum percent entrapment efficiency (97.09 ± 0.11%) was selected as optimized formulation. In case of liposomes, formulation F12 was selected. Patches loaded with niosomes showed 95.12 ± 1.19% cumulative amount of drug permeated as compared to liposomal vesicle-loaded patches which showed 82.21 ± 1.24% and control patches 70.10 ± 1.33%. DISCUSSION: Flux, permeation rate and permeability coefficient were found to be higher in case of niosomal patches as compared to liposomal patches and control patches. Surfactant present in niosomes act as a penetration enhancer which contribute in the permeation enhancement of buflomedil hydrochloride from niosomes. CONCLUSION: Thus, it was concluded that niosomal vesicles represented to be an efficient and stable vesicular carrier for transdermal delivery of buflomedil hydrochloride.

Interpenetrating polymer networks as innovative drug delivery systems.

Polymers have always been valuable excipients in conventional dosage forms, also have shown excellent performance into the parenteral arena, and are now capable of offering advanced and sophisticated functions such as controlled drug release and drug targeting. Advances in polymer science have led to the development of several novel drug delivery systems. Interpenetrating polymer networks (IPNs) have shown superior performances over the conventional individual polymers and, consequently, the ranges of applications have grown rapidly for such class of materials. The advanced properties of IPNs like swelling capacity, stability, biocompatibility, nontoxicity and biodegradability have attracted considerable attention in pharmaceutical field especially in delivering bioactive molecules to the target site. In the past few years various research reports on the IPN based delivery systems showed that these carriers have emerged as a novel carrier in controlled drug delivery. The present review encompasses IPNs, their types, method of synthesis, factors which affects the morphology of IPNs, extensively studied IPN based drug delivery systems, and some natural polymers widely used for IPNs.

Carbon nanotubes: an emerging drug carrier for targeting cancer cells.

During recent years carbon nanotubes (CNTs) have been attracted by many researchers as a drug delivery carrier. CNTs are the third allotropic form of carbon-fullerenes which were rolled into cylindrical tubes. To be integrated into the biological systems, CNTs can be chemically modified or functionalised with therapeutically active molecules by forming stable covalent bonds or supramolecular assemblies based on noncovalent interactions. Owing to their high carrying capacity, biocompatibility, and specificity to cells, various cancer cells have been explored with CNTs for evaluation of pharmacokinetic parameters, cell viability, cytotoxicty, and drug delivery in tumor cells. This review attempts to highlight all aspects of CNTs which render them as an effective anticancer drug carrier and imaging agent. Also the potential application of CNT in targeting metastatic cancer cells by entrapping biomolecules and anticancer drugs has been covered in this review.

Physicochemical and pharmacological investigation of water/oil microemulsion of non-selective beta blocker for treatment of glaucoma.

PURPOSE: Ocular drug delivery system always remained associated with lots of difficulties and faced issues of poor drug absorption and poor bioavailability. Timolol maleate is a nonspecific beta blocker used for reduction of elevated intraocular pressure in glaucoma. Timolol maleate is absorbed systemically and is contraindicated in asthmatic patients. This study is focused to deliver Timolol maleate by a water/oil microemulsion to extend the time of reduced intraocular pressure of glaucomatous rabbit's eye measured by using a Schoetz tonometer. METHODS: The microemulsion is prepared by mixing the oily components with two nonionic surfactants, drug and water, and evaluated for the physicochemical, in vitro and in vivo parameters. RESULTS: The colloidal system demonstrates monodisperse distribution behavior and exhibits a uniform size distribution of finite width. In vitro drug release from microemulsion was found to follow Higuchi's pattern followed by a zero-order drug release by the emulsion. Ex vivo permeation through goat cornea revealed delayed release of Timolol maleate from microemulsion as compared with its aqueous solution. A reduction in intraocular pressure is seen lasting for 12 h compared to aqueous eye drop that lasted for only 5 h. CONCLUSION. In vivo reduction of intraocular pressure revealed a similar efficacy for once daily dosed 0.3% Timolol maleate in microemulsion formulation compared to 0.5% concentration in both microemulsion as well as aqueous formulation. The possible outcome of dose reduction will reduce the cardiovascular side effects generally reported with Timolol maleate eye drops.

Tranexamic acid loaded gellan gum-based polymeric microbeads for controlled release: in vitro and in vivo assessment.

Gellan gum (GG) microbeads containing tranexamic acid (TA), an anti-fibrinolytic drug were prepared by a classic sol-gel transition induced by ionic crosslinking technique using aluminum chloride (AlCl3) as cross-linking agent. The influence of different formulation variables on in vitro physico-chemical parameters and drug release studies were performed systematically. The microbeads were evaluated by scanning electron microscopy (SEM), Fourier transform infra-red (FTIR) spectroscopy, X-ray diffraction (XRD), differential scanning calorimetry (DSC) and high performance liquid chromatographic (HPLC) analysis. Particle size and swelling behavior of microbeads were also investigated. Microbeads showed improved drug encapsulation efficiency along with enhanced drug release. The in vivo studies exhibited sustained drug release in rabbits over a prolonged period after oral administration of these newly developed TA loaded GG microbeads. Based on the results of in vitro and in vivo studies in experimental animal model it was concluded that these microbeads provided intestinal specific controlled release of TA.

Preparation and in vitro evaluation of xanthan gum facilitated superabsorbent polymeric microspheres.

Interpenetrating polymer network (IPN) hydrogel microspheres of xanthan gum (XG) based superabsorbent polymer (SAP) and poly(vinyl alcohol) (PVA) were prepared by water-in-oil (w/o) emulsion crosslinking method for sustained release of ciprofloxacin hydrochloride (CIPRO). The microspheres were prepared with various ratios of hydrolyzed SAP to PVA and extent of crosslinking density. The prepared microspheres with loose and rigid surfaces were evidenced by scanning electron microscope (SEM). Fourier transform infrared spectroscopy (FTIR) and X-ray diffraction (XRD) analysis confirmed the IPN formation. Differential scanning calorimetry (DSC) study was performed to understand the dispersion nature of drug after encapsulation. The in vitro drug release study was extensively evaluated depending on the process variables in both acidic and alkaline media. All the formulations exhibited satisfactory physicochemical and in vitro release characteristics. Release data indicated a non-Fickian trend of drug release from the formulations. Based on the results, this study suggest that CIPRO loaded IPN microspheres were suitable for sustained release application.

Design expert supported mathematical optimization and predictability study of buccoadhesive pharmaceutical wafers of Loratadine.

OBJECTIVE: The objective of this work encompasses the application of the response surface approach in the development of buccoadhesive pharmaceutical wafers of Loratadine (LOR). METHODS: Experiments were performed according to a 3(2) factorial design to evaluate the effects of buccoadhesive polymer, sodium alginate (A), and lactose monohydrate as ingredient, of hydrophilic matrix former (B) on the bioadhesive force, disintegration time, percent (%) swelling index, and time taken for 70% drug release (t(70%)). The effect of the two independent variables on the response variables was studied by response surface plots and contour plots generated by the Design-Expert software. The desirability function was used to optimize the response variables. RESULTS: The compatibility between LOR and the wafer excipients was confirmed by differential scanning calorimetry, FTIR spectroscopy, and X-ray diffraction (XRD) analysis. Bioadhesion force, measured with TAXT2i texture analyzer, showed that the wafers had a good bioadhesive property which could be advantageous for retaining the drug into the buccal cavity. CONCLUSION: The observed responses taken were in agreement with the experimental values, and Loratadine wafers were produced with less experimental trials, and a patient compliant product was achieved with the concept of formulation by design.

A RP-HPLC method for quantification of diclofenac sodium released from biological macromolecules.

Interpenetrating network (IPN) microbeads of sodium carboxymethyl locust bean gum (SCMLBG) and sodium carboxymethyl cellulose (SCMC) containing diclofenac sodium (DS), a nonsteroidal anti-inflammatory drug, were prepared by single water-in-water (w/w) emulsion gelation process using AlCl3 as cross-linking agent in a complete aqueous environment. Pharmacokinetic study of these IPN microbeads was then carried out by a simple and feasible high-performance liquid chromatographic method with UV detection which was developed and validated for the quantification of diclofenac sodium in rabbit plasma. The chromatographic separation was carried out in a Hypersil BDS, C18 column (250 mm × 4.6 mm; 5 m). The mobile phase was a mixture of acetonitrile and methanol (70:30, v/v) at a flow rate of 1.0 ml/min. The UV detection was set at 276 nm. The extraction recovery of diclofenac sodium in plasma of three quality control (QC) samples was ranged from 81.52% to 95.29%. The calibration curve was linear in the concentration range of 20-1000 ng/ml with the correlation coefficient (r(2)) above 0.9951. The method was specific and sensitive with the limit of quantification of 20 ng/ml. In stability tests, diclofenac sodium in rabbit plasma was stable during storage and assay procedure.

Trivalent ion cross-linked pH sensitive alginate-methyl cellulose blend hydrogel beads from aqueous template.

pH sensitive alginate-methyl cellulose blend hydrogel beads were prepared by single water-in-water (w/w) emulsion gelation method in a complete aqueous environment. The influence of different variables like total polymer concentration, gelation time and crosslinker content on in vitro physico-chemical characteristics and drug release rate in different medium were investigated. Drug loaded beads were evaluated through Fourier Transform Infra-red (FTIR), X-ray diffraction (XRD) and Differential Scanning Calorimetry (DSC) analysis. Scanning electron microscopy (SEM) picture of the dried beads suggested the formation of hemispherical particles. FTIR analysis indicated the stable nature of the drug in the blend hydrogel beads. DSC and XRD analysis revealed amorphous state of drug after encapsulation. The drug release profile in acidic medium was considerably less in compared in alkaline media. Formulations showed non-Fickian type transport mechanism. This trivalent ion crosslinked beads not only improves drug encapsulation efficiency but also enhances drug release in alkaline media.

Al3+ ion cross-linked interpenetrating polymeric network microbeads from tailored natural polysaccharides.

Interpenetrating network (IPN) microbeads of sodium carboxymethyl locust bean gum (SCMLBG) and sodium carboxymethyl cellulose (SCMC) containing diclofenac sodium (DS), a non steroidal anti-inflammatory drug were prepared by single water-in-water (w/w) emulsion gelation process using AlCl(3) as cross-linking agent in a complete aqueous environment. The influence of different variables like total polymer concentration, gelation time and crosslinker content on in vitro physico-chemical characteristics and drug release rate in different media was investigated. Drug loaded microbeads were evaluated through Fourier transform infra-red (FTIR), X-ray diffraction (XRD) and differential scanning calorimetry (DSC) analyses. Scanning electron microscopy (SEM) micrograph of the beads suggested the formation of spherical particles. FTIR analysis indicated the stable nature of the drug in the blend microbeads. DSC and XRD analysis revealed amorphous state of drug after encapsulation. The drug release profile in acidic medium was considerably less in comparison to alkaline media. Formulations showed non-Fickian type transport mechanism. These tri-valent ion crosslinked beads not only improve drug encapsulation efficiency but also enhance drug release in phosphate buffer.

Interpenetrating polymer network (IPN) hydrogel microspheres for oral controlled release application.

Interpenetrating polymer network (IPN) hydrogel microspheres of sodium carboxymethyl cellulose (NaCMC) and poly(vinyl alcohol) (PVA) were prepared by water-in-oil (w/o) emulsion crosslinking method for oral controlled release delivery of a non-steroidal anti-inflammatory drug, diclofenac sodium (DS). The microspheres were prepared with various ratios of NaCMC to PVA, % drug loading and extent of crosslinking density at a fixed polymer weight. The prepared microspheres with loose and rigid surfaces were evidenced by scanning electron microscope (SEM). Fourier transform infrared spectroscopy (FTIR) and X-ray diffraction (XRD) analysis confirmed the IPN formation. Differential scanning calorimetry (DSC) study was performed to understand the dispersion nature of drug after encapsulation. The in vitro drug release study was extensively evaluated depending on the process variables in both acid and alkaline media. All the formulations exhibited satisfactory physicochemical and in vitro release characteristics. Release data indicated a non-Fickian trend of drug release from the formulations. Based on the results of this study suggest that DS loaded IPN microspheres were suitable for oral controlled release application.