Paclitaxel loaded lipid nanoemulsions for the treatment of brain tumour

Description to be added.Cannot be left empt

Liposome Delivery Systems for Inhalation: A Critical Review Highlighting Formulation Issues and Anticancer Applications

This was a critical review on research conducted in the field of pulmonary delivery of liposomes. Issues related to mechanism of the nebulization and liposome composition were appraised and correlated with the literature reports of liposome formulations used in clinical trials to understand the role of liposome size and composition on therapeutic outcome. A major highlight was the liposome inhalation for the treatment of lung cancers. Many in-vivo studies that explored the potential of liposomes as anticancer carrier systems were evaluated including animal studies and clinical trials. Liposomes can entrap anticancer drugs and localize their action in the lung following pulmonary delivery. Safety of inhaled liposomes incorporating anticancer drug depends on the anticancer agent used and the amount of drug delivered to the target cancer in the lung. The difficulty of efficient targeting of liposomal anticancer aerosols to the cancerous tissues within the lung may result in low dose reaching the target site. Overall, following the success of liposomes as inhalable carriers in the treatment of lung infections, it is expected that more focus from research and development will be given to designing inhalable liposome carriers for the treatment of other lung diseases including pulmonary cancers. Successful development of anticancer liposomes for inhalation may depend on future development of effective aerosolization devices and better targeted liposomes to maximize benefit of therapy and reduce potential of local and systemic adverse effects

Amine functionalization of cholecyst-derived extracellular matrix with generation 1 PAMAM dendrimer

This document is the unedited author's version of a Submitted Work that was subsequently accepted for publication in Biomacromolecules, copyright © American Chemical Society after peer review. To access the final edited and published work, see http://pubs.acs.org/doi/pdf/10.1021/bm701055k.A method to functionalize cholecyst-derived extracellular matrix (CEM) with free amine groups was established in an attempt to improve its potential for tethering of bioactive molecules. CEM was incorporated with Generation-1 polyamidoamine (G1 PAMAM) dendrimer by using N-(3-dimethylaminopropyl)-N′-ethylcarbodiimide and N-hydroxysuccinimide cross-linking system. The nature of incorporation of PAMAM dendrimer was evaluated using shrink temperature measurements, Fourier transform infrared (FTIR) assessment, ninhydrin assay, and swellability. The effects of PAMAM incorporation on mechanical and degradation properties of CEM were evaluated using a uniaxial mechanical test and collagenase degradation assay, respectively. Ninhydrin assay and FTIR assessment confirmed the presence of increasing free amine groups with increasing quantity of PAMAM in dendrimer-incorporated CEM (DENCEM) scaffolds. The amount of dendrimer used was found to be critical in controlling scaffold degradation, shrink temperature, and free amine content. Cell culture studies showed that fibroblasts seeded on DENCEM maintained their metabolic activity and ability to proliferate in vitro. In addition, fluorescence cell staining and scanning electron microscopy analysis of cell-seeded DENCEM showed preservation of normal fibroblast morphology and phenotype

An Ethanol-Based Proliposome Technology for Enhanced Delivery and Improved Respirability of Antiasthma Aerosols Generated Using a Micropump Vibrating-Mesh Nebulizer

Salbutamol sulphate liposomes were generated using ethanolbased proliposomes followed by nebulization using an Aeroneb Pro vibrating-mesh nebulizer. The droplet size, output and fine particle fraction (FPF) of the drug incorporated in liposome formulation were compared to those of a conventional drug solution. Aerosol output was determined gravimetrically and drug output was analyzed by using high performance liquid chromatography. The potential of aerosol deposition in deep lung was evaluated using inertial impaction and laser diffraction. The effect of formulation surface tension on the aerosol performance was studied. Output and FPF were improved using liposomes compared to the conventional solution, for instance, FPF values were 57.85% and 45.81% respectively. The volume median diameter as measured by laser diffraction was respectively 3.44 μm and 3.22 μm; however, the higher FPF of the liposome formulation is justified by the lower polydispersity of its aerosol. The improved aerosol performance using liposomes was attributed to the reduction of surface tension caused by the presence of phospholipid. This is the first study that demons trates the ability of liposomes to improve the nebulized drug output and FPF

Proliposome powder or tablets for generating inhalable liposomes using a medical nebulizer

Purpose: The aim of this study was to develop and compare proliposome powder and proliposome tablet formulations for drug delivery from a Pari-LC Sprint nebulizer. Methods: Proliposome powders were prepared by the slurry method and sorbitol or mannitol carbohydrate carrier were used in a 1:10 and 1:15 w/w lipid phase to carrier ratio. Beclometasone dipropionate (BDP; 2 mol%) was incorporated in the lipid phase. Proliposome powders were compressed into tablets, and liposomes were generated from proliposome powders or tablets within the nebulizer reservoir for subsequent aerosolization. Results: Comparatively, shorter sputtering times were reported for the tablet formulations (≈ < 2.7±0.45 min), indicating uniform aerosolization. Post-nebulization, liposomes size was larger in the nebulizer reservoir in the range of 7.79±0.48 µm–9.73±1.53 µm for both powder and tablet formulations as compared to freshly prepared liposomes (5.38±0.73 µm–5.85±0.86 µm), suggesting liposome aggregation/fusion in the nebulizer’s reservoir. All formulations exhibited more than 80% mass output regardless of formulation type, but greater BDP proportions (circa 50%) were delivered to the Two-stage Impinger when tablet formulations were used. Moreover, the nebulized droplet median size and size distribution were lower for all tablet formulations in comparison to the powder formulations. Proliposome tablet and powdered formulations demonstrated the ability to generate vesicles that sustained the release of BDP. Conclusion: Overall, this study showed that proliposome tablets could be disintegrated within a Pari-LC Sprint nebulizer to generate inhalable aerosol, with high drug output and hence can be manufactured on large scale to overcome the storage problems associated with powder formulations

Ethanol-based proliposome delivery systems of paclitaxel for in vitro application against brain cancer cells

In this study the anticancer activity of paclitaxel-loaded nano-liposomes on glioma cell lines was investigated. Soya phosphatidylcholine:cholesterol (SPC:Chol), hydrogenated soya phosphatidylcholine:cholesterol (HSPC:Chol) or dipalmitoylphosphatidylcholine:cholesterol (DPPC:Chol) in 1:1 mole ratio were used to prepare ethanol-based proliposomes. Following hydration of proliposomes, the size of resulting vesicles was subsequently reduced to nanometer scale via probe-sonication. The resulting formulations were characterized in terms of size, zeta potential and morphology of the vesicles, and entrapment efficiency of paclitaxel (PX) as well as the final pH of the preparations. DPPC-liposomes entrapped 35–92% of PX compared to 27–74% and 25–60% entrapped by liposomes made from SPC and HSPC formulations respectively, depending on drug concentration. The entrapment efficiency of liposomes was dependent on the lipid bilayer properties and ability of PX to modify surface charge of the vesicles. In vitro cytotoxicity studies revealed that PX-liposome formulations were more selective at inhibiting the malignant cells. The cytotoxicity of PX-liposomes was dependent on their drug-entrapment efficiency. This study has shown PX-liposomes generated from proliposomes have selective activity against glioma cell lines, and the synthetic DPPC phospholipid was most suitable for maximized drug entrapment and highest activity against the malignant cells in vitro

Spray-Dried Proliposome Microparticles for High-Performance Aerosol Delivery Using a Monodose Powder Inhaler

Proliposome formulations containing salbutamol sulphate (SS) were developed using spray drying, and the effects of carrier type (lactose monohydrate (LMH) or mannitol) and lipid to carrier ratio were evaluated. The lipid phase comprised soy phosphatidylcholine (SPC) and cholesterol (1:1), and the ratios of lipid to carrier were 1:2, 1:4, 1:6, 1:8 or 1:10 w/w. X-ray powder diffraction (XRPD) revealed an interaction between the components of the proliposome particles, and scanning electron microscopy (SEM) showed that mannitol-based proliposomes were uniformly sized and spherical, whilst LMH-based proliposomes were irregular and relatively large. Using a two-stage impinger (TSI), fine particle fraction (FPF) values of the proliposomes were higher for mannitol-based formulations, reaching 52.6%, which was attributed to the better flow properties when mannitol was used as carrier. Following hydration of proliposomes, transmission electron microscopy (TEM) demonstrated that vesicles generated from mannitol-based formulations were oligolamellar, whilst LMH-based proliposomes generated ‘worm-like’ structures and vesicle clusters. Vesicle size decreased upon increasing carrier to lipid ratio, and the zeta potential values were negative. Drug entrapment efficiency (EE) was higher for liposomes generated from LMH-based proliposomes, reaching 37.76% when 1:2 lipid to carrier ratio was used. The in vitro drug release profile was similar for both carriers when 1:6 lipid to carrier ratio was used. This study showed that spray drying can produce inhalable proliposome microparticles that can generate liposomes upon contact with an aqueous phase, and the FPF of proliposomes and the EE offered by liposomes were formulation-dependent

Proteína G - mecanismos moleculares de comunicação celular

In the present paper the authors commnent on the physiological role of G proteins in transmission signalling process and some alterations of this system. The review is directed to beginners and emphasize a visual approach to the theme.No presente artigo os autores comentam o papel fisiológico das proteínas G no processo de sinalização de transmissão e algumas alterações desses sistemas. A revisão é dirigida a iniciantes e enfatizar uma abordagem visual para o tema

INOVASI SIPAKAMASETA UNTUK MENDORONG LITERASI DIGITALISASI DI DESA TAMANNYELENG, KABUPATEN GOWA, SULAWESI SELATAN

Technology is increasingly being used in governance, especially in sub-districts and rural areas, to improve community services and reduce the perception of rural backwardness. However, there are challenges in the development of digital villages, including a lack of understanding of technology and limited utilization. To overcome this, the community service team of Hasanuddin University made an innovation of the SIPAKAMASETA program as a form of community service carried out in Tamnyeleng Village, Gowa Regency, South Sulawesi. The method used in this program consists of four stages, namely material and data collection, manufacturing, testing, and training. The stages in this method involve the initial assessment of digital literacy and community needs (pre-test), program implementation (village service website and digital literacy corner) as well as evaluation (post-test), and monitoring. This program provides significant benefits to the local community and has succeeded in making Tamannyeleng Village a digital village. This is reflected through the existence of websites that support community services, especially in administration and digital literacy corners as centers of activity and training that have increased people\u27s knowledge and skills related to the world of digitalization and technology that can improve the quality of life of the community.  ---  Teknologi semakin banyak digunakan dalam pemerintahan, terutama di kecamatan dan pedesaan, untuk meningkatkan layanan masyarakat dan mengurangi persepsi keterbelakangan pedesaan. Namun, terdapat tantangan dalam pengembangan desa digital, antara lain kurangnya pemahaman terhadap teknologi dan pemanfaatan yang terbatas. Untuk mengatasi hal tersebut, tim pengabdian masyarakat Universitas Hasanuddin membuat inovasi program SIPAKAMASETA sebagai bentuk pengabdian masyarakat yang dilaksanakan di Desa Tamnyeleng, Kabupaten Gowa, Sulawesi Selatan. Metode yang digunakan dalam program ini terdiri dari empat tahap, yaitu pengumpulan materi dan data, pembuatan, pengujian, dan pelatihan. Tahapan dalam metode ini meliputi penilaian awal literasi digital dan kebutuhan masyarakat (pre-test), pelaksanaan program (website layanan desa dan pojok literasi digital) serta evaluasi (post-test) dan monitoring. Program ini memberikan manfaat yang signifikan bagi masyarakat setempat dan berhasil menjadikan Desa Tamannyeleng sebagai desa digital. Hal ini tercermin melalui keberadaan website yang mendukung pengabdian masyarakat, khususnya di bidang administrasi dan pojok literasi digital sebagai pusat kegiatan dan pelatihan yang telah meningkatkan pengetahuan dan keterampilan masyarakat terkait dunia digitalisasi dan teknologi yang dapat meningkatkan kualitas hidup masyarakat

Cyclodextrin Diethyldithiocarbamate Copper II Inclusion Complexes: A Promising Chemotherapeutic Delivery System against Chemoresistant Triple Negative Breast Cancer Cell Lines

Diethyldithiocarbamate Copper II (DDC-Cu) has shown potent anticancer activity against a wide range of cancer cells, but further investigations are hindered by its practical insolubility in water. In this study, inclusion complexes of DDC-Cu with hydroxypropyl beta-cyclodextrin (HP) or sulfobutyl ether beta-cyclodextrin (SBE) were prepared and investigated as an approach to enhance the apparent solubility of DDC-Cu. Formulations were prepared by simple mixing of DDC-Cu with both cyclodextrin (CDs) at room temperature. Phase solubility assessments of the resulting solutions were performed. DDC-Cu CD solutions were freeze-dried for further characterisations by DSC, thermogravimetric analysis (TGA) and FT-IR. Stability and cytotoxicity studies were also performed to investigate the maintenance of DDC-Cu anticancer activity. The phase solubility profile deviated positively from the linearity (Ap type) showing significant solubility enhancement of the DDC-Cu in both CD solutions (approximately 4 mg/mL at 20% w/w CD solutions). The DSC and TGA analysis confirmed the solid solution status of DDC-Cu in CD. The resulting solutions of DDC-Cu were stable for 28 days and conveyed the anticancer activity of DDC-Cu on chemoresistant triple negative breast cancer cell lines, with IC50 values less than 200 nM. Overall, cyclodextrin DDC-Cu complexes offer a great potential for anticancer applications, as evidenced by their very positive effects against chemoresistant triple negative breast cancer cells