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Luca Ivan Ardolino, Marisa Meloni, Giuseppe Brugali, Emanuela Corsini, Corrado Lodovico Galli
BACKGROUND: Polybactum (Effik International, Brussels, Belgium) is a vaginal mucoadhesive product (medical device) designed to form a film that acts as a mechanical barrier with the aim of inhibiting colonization by specific pathogens. It contains polycarbophil, a bioadhesive agent, and lauryl glucoside (LG), a nonionic surfactant that reinforces the barrier effect through its tensioactive properties. OBJECTIVE: To assess the local safety profile, tolerability, and efficacy of Polybactum formulations...
2016: Current Therapeutic Research, Clinical and Experimental
Guoxin Tan, Shihui Yu, Hao Pan, Jinyu Li, Dandan Liu, Kun Yuan, Xinggang Yang, Weisan Pan
The aim of this study was to develop and characterize a novel colloidal system, namely, timolol maleate chitosan coated liposomes (TM-CHL) to enhance the ocular permeation, precorneal residence time and bioavailability. The resulting TM-CHL was the most promising formulation with a mean particle size of 150.7nm and an EE% of 75.83±1.61%. In vitro release of the TM-CHL showed an extended drug release profile. The TM-CHL exhibited significant mucin adhesion and compared with commercial eye drops, TM-CHL produced a 3...
October 17, 2016: International Journal of Biological Macromolecules
Kira S Zadesenets, Dita B Vizoso, Aline Schlatter, Irina D Konopatskaia, Eugene Berezikov, Lukas Schärer, Nikolay B Rubtsov
Over the past decade, the free-living flatworm Macrostomum lignano has been successfully used in many areas of biology, including embryology, stem cells, sexual selection, bioadhesion and aging. The increased use of this powerful laboratory model, including the establishment of genomic resources and tools, makes it essential to have a detailed description of the chromosome organization of this species, previously suggested to have a karyotype with 2n = 8 and one pair of large and three pairs of small metacentric chromosomes...
2016: PloS One
Hao Meng, Yuan Liu, Bruce P Lee
: Mussel adhesive moiety, catechol, has been utilized to design a wide variety of biomaterials. However, the biocompatibility and biological responses associated with the byproducts generated during the curing process of catechol has never been characterized. An in situ curable polymer model system, 4-armed polyethylene glycol polymer end-capped with dopamine (PEG-D4), was used to characterize the production of hydrogen peroxide (H2O2) during the oxidative crosslinking of catechol. Although PEG-D4 cured rapidly (under 30s), catechol continues to polymerize over several hours to form a more densely crosslinked network over time...
October 12, 2016: Acta Biomaterialia
Chu Gong, Caicai Lu, Bingqiang Li, Meng Shan, Guolin Wu
Hydrogel systems based on cross-linked polymeric materials with adhesive properties in wet environments have been considered as promising candidates for tissue adhesives. The 3,4-dihydroxyphenylalanine (DOPA) is believed to be responsible for the water-resistant adhesive characteristics of mussel adhesive proteins. Under the inspiration of DOPA containing adhesive proteins, a dopamine-modified poly(α,β-aspartic acid) derivative (PDAEA) was successfully synthesized by successive ring-opening reactions of polysuccinimide (PSI) with dopamine and ethanolamine, and an injectable bioadhesive hydrogel was prepared via simply mixing PDAEA and FeCl3 solutions...
October 14, 2016: Journal of Biomedical Materials Research. Part A
Juntao Yin, Cuiyu Xiang, Guangxiu Lu
Palmatine (PM) is a potent anti-infective agent used to treat eye diseases. However, PM is less effective for ocular application due to short residence time within the eyes. This study aimed to develop a cationic lipid emulsions (CLEs) for ophthalmic delivery of PM and evaluate its suitability in infection treatment. PM-loaded CLEs (PM-CLEs) were prepared through emulsifying/high pressure homogenization and characterized by particle size, ζ potential and morphology. The resulting PM-CLEs possessed a particle size of 192 nm and ζ potential of 45 mV around...
October 13, 2016: Journal of Microencapsulation
Sara Pistone, Francisco M Goycoolea, Alix Young, Gro Smistad, Marianne Hiorth
The efficacy of treatments for oral ailments is often challenged by a low residence time of the conventional pharmaceutical formulations in the oral cavity. The residence time in the oral cavity could be improved by using bioadhesive formulations, such as preparations based on polysaccharides. This study describes the formulation and the evaluation of polysaccharide-based nanosystems as drug delivery systems addressed to the oral cavity. Nanoparticles based on chitosan, alginate or pectin were prepared through self-assembly by ionotropic gelation using oppositely charged crosslinkers (tripolyphosphate or zinc)...
October 6, 2016: European Journal of Pharmaceutical Sciences
Jianing Meng, Vivek Agrahari, Miezan J Ezoulin, Chi Zhang, Sudhaunshu S Purohit, Agostino Molteni, Daniel Dim, Nathan A Oyler, Bi Botti C Youan
It is hypothesized that a thiolated chitosan (TCS) core/shell nanofiber (NF) can enhance the drug loading of tenofovir, a model low molecular weight and highly water soluble drug molecule, improve its mucoadhesivity, and in vivo safety. To test this hypothesis, PEO core with TCS shell NFs are fabricated by a coaxial electrospinning technique. The morphology, drug loading, drug release profiles, cytotoxicity and mucoadhesion of the NFs are analysised using scanning and transmission electron microscopies, liquid chromatography, cytotoxicity assays on VK2/E6E7 and End1/E6E7 cell lines and Lactobacilli crispatus, and periodic acid colorimetric method, respectively...
October 4, 2016: Molecular Pharmaceutics
Emil Meng-Lund, Jette Jacobsen, Anette Müllertz, Erling B Jørgensen, René Holm
Buccal delivery may be clinically beneficial for compounds with a high gastrointestinal and hepatic first pass metabolism or in situations where a fast systemic absorption is desired. The delivery of a crystalline low soluble compounds, e.g. diazepam, may be limited due to the low volume of saliva available to facilitate solvation in order to drive the permeation of drug through the buccal mucosa. Therefore, the present study investigated the potential benefits of administering diazepam either as an amorphous or as a crystalline form in mucoadhesive tablets to conscious Göttingen mini-pigs...
September 30, 2016: International Journal of Pharmaceutics
Deep Pooja, Hitesh Kulhari, Madhusudana Kuncha, Shyam Sunder Rachamalla, David J Adams, Vipul Bansal, Ramakrishna Sistla
Oral delivery of anticancer drugs remains challenging despite the most convenient route of drug administration. Hydrophobicity and non-specific toxicities of anticancer agents are major impediments in the development of oral formulation. In this study, we developed wheat germ agglutinin (WGA)-conjugated, solid lipid nanoparticles to improve the oral delivery of the hydrophobic anticancer drug, paclitaxel (PTX). This study was focused to improve the PTX loading in biocompatible lipid matrix with high bioconjugation efficiency...
October 3, 2016: Molecular Pharmaceutics
Yang Deng, Fan Yang, Emiliano Cocco, Eric Song, Junwei Zhang, Jiajia Cui, Muneeb Mohideen, Stefania Bellone, Alessandro D Santin, W Mark Saltzman
The i.p. administration of chemotherapy in ovarian and uterine serous carcinoma patients by biodegradable nanoparticles may represent a highly effective way to suppress peritoneal carcinomatosis. However, the efficacy of nanoparticles loaded with chemotherapeutic agents is currently hampered by their fast clearance by lymphatic drainage. Here, we show that a unique formulation of bioadhesive nanoparticles (BNPs) can interact with mesothelial cells in the abdominal cavity and significantly extend the retention of the nanoparticles in the peritoneal space...
October 11, 2016: Proceedings of the National Academy of Sciences of the United States of America
Bruno Fonseca-Santos, Aline Martins Dos Santos, Camila Fernanda Rodero, Maria Palmira Daflon Gremião, Marlus Chorilli
From previous studies, it has been found that curcumin exhibits an anti-inflammatory activity and is being used for the treatment of skin disorders; however, it is hydrophobic and has weak penetrating ability, resulting in poor drug transport through the stratum corneum. The aim of this study was to develop liquid crystalline systems for topical administration of curcumin for the treatment of inflammation. These liquid crystalline systems were developed from oleic acid, polyoxypropylene (5) polyoxyethylene (20) cetyl alcohol, and water as the surfactant, oil phase, and aqueous phase, respectively...
2016: International Journal of Nanomedicine
Marcela P Tedesco, Carla A Monaco-Lourenço, Rosemary A Carvalho
Oral disintegrating film represents an optimal alternative for delivery system of active compounds. The choice of film-forming polymer is the first step in the development of oral disintegrating films and the knowledge of molecular interactions in this matrix is fundamental to advance in this area. Therefore, this study aimed to characterize gelatin and hydroxypropyl methylcellulose (HPMC) films and their blends as matrices of oral disintegrating films. The films were produced by casting technique and were characterized by scanning electron microscopy, Fourier transform infrared spectroscopy, differential scanning calorimetry, mechanical properties, contact angle, time disintegration and bioadhesive strength...
December 1, 2016: Materials Science & Engineering. C, Materials for Biological Applications
Umme Hani, H G Shivakumar, Riyaz Ali M Osmani, Atul Srivastava, Naga Sravan Kumar Varma
The present investigation was designed to formulate a natural tablet for the treatment of vaginal candidiasis in order to eliminate side effects that are caused by existing antifungal drugs. Curcumin has promising antifungal activity in comparison with the existing azole antifungal drugs. Bioadhesive curcumin vaginal tablets were prepared by direct compression with different ratios of biadhesive polymers like xanthan gum, guar gum and HPMC. Curcumin tablets were characterized by studies of friability, hardness, hydration, DSC, mucoadhesion, In-vitro release and antifungal activity...
2016: Iranian Journal of Pharmaceutical Research: IJPR
Vaishali Thakkar, Vaishali Korat, Lalji Baldaniya, Mukesh Gohel, Tejal Gandhi, Nirav Patel
INTRODUCTION: The aim of burn management and therapy is fast healing and epithelisation to prevent infection. The present study is concerned with the development and characterization of a novel nanaoparticulate system; cubosomes, loaded with silver sulfadiazine (SSD) and Aloe vera for topical treatment of infected burns. METHODS: Cubosome dispersions were formulated by an emulsification technique using different concentrations of a lipid phase Glyceryl Monooleate (GMO) and Poloxamer 407...
July 2016: International Journal of Pharmaceutical Investigation
Benjamin O Emikpe, Victor O Oyebanji, Michael A Odeniyi, Adebayo M Salaam, Omolade A Oladele, Theophilus A Jarikre, Oluwole A Akinboade
BACKGROUND: Few studies have investigated the interaction of bioadhesives with biologic tissues for veterinary application. Hence, this study evaluates the mucoadhesive property and vaccine delivery properties of polymers from phytogenic origin. Gums from Cedrela odorata and Khaya senegalensis were harvested, purified, dried and compressed into 500 mg tablets individually and in combined ratios. The time taken for these tablets, placed on freshly excised (5 × 5 cm) trachea and duodenal tissues of cattle, chicken, pig, sheep and goat and fastened to the basket end of a tablet dissolution machine probe set at 50 rev/min in a phosphate buffer 6...
2016: SpringerPlus
F Scognamiglio, A Travan, M Borgogna, I Donati, E Marsich, J W A M Bosmans, L Perge, M P Foulc, N D Bouvy, S Paoletti
UNLABELLED: An emerging strategy to improve adhesiveness of biomaterials in wet conditions takes inspiration from the adhesive features of marine mussel, which reside in the chemical reactivity of catechols. In this work, a catechol-bearing molecule (dopamine) was chemically grafted onto alginate to develop a polysaccharide-based membrane with improved adhesive properties. The dopamine-modified alginates were characterized by NMR, UV spectroscopy and in vitro biocompatibility. Mechanical tests and in vitro adhesion studies pointed out the effects of the grafted dopamine within the membranes...
October 15, 2016: Acta Biomaterialia
T S Anirudhan, Syam S Nair, Anoop S Nair
A novel efficient transdermal (TD) lidocaine (LD) delivery device based on chitosan (CS) and hyaluronic acid (HA) was successfully developed in the present investigation. CS was grafted with glycidyl methacrylate (GMA) and butyl methacrylate (BMA) to fabricate a versatile material with improved adhesion and mechanical properties. HA was hydrophobically modified by covalently conjugating 3-(dimethylamino)-1-propylamine (DMPA) to encapsulate poorly water soluble LD and was uniformly dispersed in modified CS matrix...
November 5, 2016: Carbohydrate Polymers
Seonki Hong, David Pirovich, Aoife Kilcoyne, Chen-Han Huang, Hakho Lee, Ralph Weissleder
A novel metallo-bioadhesive to be used as tissue sealant in minimally invasive procedures is reported. Metal complexation can be used to render gelatin derivatives adhesive, which occurs in minutes, is efficient, and fully biodegradable within weeks.
October 2016: Advanced Materials
Prakash Namdeo Kendre, Pravin Digambar Chaudhari
The present study involved the design and development of oral bioadhesive pellets of eplerenone. A solid dispersion of eplerenone was developed with a hydrophilic carrier, polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer (Soluplus®). Bioadhesive pellets were prepared from this solid dispersion using a combination of HPMC K4M and Carbopol 934P. Both the solid dispersion and the pellets were evaluated for various physicochemical properties such as solubility, entrapment efficiency, drug content, surface morphology, mucoadhesion and swelling behaviour...
August 5, 2016: Drug Development and Industrial Pharmacy
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