Intranasal niosomes of nefopam with improved bioavailability: preparation, optimization, and in-vivo evaluation

Heba A Abou-Taleb,1 Rasha A Khallaf,2 Jelan A Abdel-Aleem3 1Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Nahda University (NUB), Beni Suef, Egypt; 2Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Beni-Suef University, Beni Suef, Egypt; 3Department of Industrial Pharmacy, Faculty of Pharmacy, Assiut University, Assiut, Egypt Objective: One of the greatest challenges drug formulation is facing is poor bioavailability via oral route. In this regard, nasal drug delivery has been commonly used as an alternative route to improve drug bioavailability. Nefopam hydrochloride (NF) is an analgesic drug that suffers from poor bioavailability due to extensive metabolism in liver. Accordingly, the goal of the present study was to improve NF bioavailability via niosomal-based formulation designed for intranasal delivery.Materials and methods: Vesicles were developed by mixing surfactants (Span 20, Span 40, Span 80, and Span 85) at four molar ratios of 1:1, 1:2, 1:3, and 1:4 of cholesterol to surfactant. Entrapment efficiency, particle size, zeta potential, release percentage, ex-vivo permeation parameters, and niosomes’ stability were determined. Also, the pharmacokinetic parameters of the optimized formula in in-situ gel base were measured in rats.Results: Niosomes showed entrapment efficiency >80%, particle size <550 nm, and zeta potential ranging from -16.8±0.13 to -29.7±0.15. The produced vesicles showed significantly higher amounts of drug permeated across nasal mucosa (2.5 folds) and prolonged NF release compared with NF solution. Stability studies of optimum formula showed nonsignificant changes in niosomes parameters over a storage period of 6 months. The in-vivo studies showed a 4.77-fold increase in bioavailability of optimized nasal niosomes compared with oral solution of drug.Conclusion: The obtained results revealed the great ability of the produced NF-loaded niosomes to enhance drug penetration through nasal mucosa and improve its relative bioavailability compared with NF oral solution. Keywords: nefopam hydrochloride, intranasal permeation, niosomes, optimization, nonopioid analgesic

Study of the physico-chemical conditions and evaluation of the changes in eutrophication-related problems in El- Mex Bay

El- Mex Bay is a relatively large coastal embayment west of Alexandria. The bay is an important fishery ground as well as recreation area. It includes both the Western Harbor and Dekhaila Harbor. It is one of heavily polluted areas on the Egyptian Mediterranean coast, receiving huge amount of agricultural, industrial, and sewage wastes from the adjacent Lake Mariut through El- Umoum Drain. According to different estimations in literatures the volume of the wastewaters varied between 7 × 106 and 8 × 106 m3day-1, which is supposed to increase with the growing population density of Alexandria city. These conditions cause pronounced eutrophication and drastic changes. Eutrophication-related problems in El- Mex Bay of Alexandria were studied seasonally from autumn 2011 to autumn 2012. Geographical information system (GIS) and remote sensing techniques were used together with the ground-based surveys to assess the vulnerability of the most important physical and eutrophication parameters along El- Mex Bay coast. As a result of increasing population and industrial development, poorly untreated industrial waste, domestic sewage, shipping industry and agricultural runoff are being released to the bay. With the rapid increase in the industries and population, changes in water quality would have potential consequences for the large rapidly growing population of the Alexandria region. Recom-mendations for environmental recovery and restoration are proposed for preservation of El- Mex Bay and harbors in order to facilitate development of environmental and tourist activities.Key words: El- Mex Bay, recreation area, El- Umoum drain, geographical information system (GIS), remote sensing, eutrophication, and restoration

Formulation and evaluation of simvastatin polymeric nanoparticles loaded in hydrogel for optimum wound healing purpose

Usama Farghaly Aly,1 Heba A Abou-Taleb,2 Ahmed AH Abdellatif,3,4 Nahla Sameh Tolba21Department of Pharmaceutics, Faculty of Pharmacy, Minia University, EL-Minia, Egypt; 2Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Nahda University (NUB), Beni-Suef, Egypt; 3Department of Pharmaceutics, College of Pharmacy, Qassim University, Al Qassim, Kingdom of Saudi Arabia; 4Department of Pharmaceutics and Industrial Pharmacy, Al-Azhar University, Assiut, Egypt Purpose: The aim of this study was to formulate a hydrogel loaded with polymeric nanoparticles (PoNPs) of simvastatin (SIM) for topical wound healing application. Materials and methods: The SIM PoNPs were prepared by using the nanoprecipitation method to improve the drug solubility and skin permeation. Furthermore, drug content, solubility, particle size, surface charge, and transmission electron microscopy of the prepared PoNPs were evaluated. Then, the PoNPs were loaded on hydrogel, and physical characteristics, in vitro release, and ex vivo permeation of the hydrogel were evaluated. Finally, the prepared gel was applied on rat wounds, and a histopathological study was performed. Results: The results showed that the drug content in the PoNPs was 86.4%. The PoNPs were spherical in shape with a smooth surface and a uniform size distribution. The particle size was 268.4±2.6, polydispersity index was ≤0.302, and zeta potential was -33±1.67 mV. The hydrogel loaded with SIM PoNPs was homogenous, and the pH was accepted and compatible with the skin. Moreover, the viscosity and spreadability assured its ease of application. The drug content was 97.25±0.02%. Furthermore, about 81% of SIM was released within 24 hours, while in the ex vivo permeation study 69.19% of SIM passed through the skin after 24 hours. Finally, the histopathological studies confirmed the efficacy of the SIM PoNPs-loaded hydrogel in wound healing due to the formation of the normal epithelial layer on day 11 after wound creation.Conclusion: The hydrogel loaded with SIM PoNPs showed a good efficacy in accelerating the healing of the rat wound with complete epithelialization and minimal inflammatory cell infiltration. Keywords: simvastatin, Carbopol® gel, ex vivo permeation, nanoprecipitaion method, wound healin

Stereo-image normalization of voluminous objects improves textile defect recognition

The visual detection of defects in textiles is an important application in the textile industry. Existing systems require textiles to be spread flat so they appear as 2D surfaces, in order to detect defects. In contrast, we show classification of textiles and textile feature extraction methods, which can be used when textiles are in inhomogeneous, voluminous shape. We present a novel approach on image normalization to be used in stain-defect recognition. The acquired database consist of images of piles of textiles, taken using stereo vision. The results show that a simple classifier using normalized images outperforms other approaches using machine learning in classification accuracy