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Eudragit^®-PEG Nanoparticles: Physicochemical Characterization and Interfacial Tension Measurements

Open Journal of Biophysics 2024年第2期14卷 121-131页

作者： Papa Mady Sy Sidy Mouhamed Dieng Alphonse Rodrigue Djiboune Louis Augustin Diaga Diouf Boucar Ndong Gora Mbaye Mounibé Diarra laboratory of Physics and Pharmaceutical Biophysics Faculty of Medicine Pharmacy and Odontology UCAD Dakar Senegal laboratory of galenic pharmacy Faculty of Medicine Pharmacy and Odontology UCAD Dakar Senegal laboratory of Medical Biophysics and Nuclear Medicine Faculty of Medicine Pharmacy and Odontology UCAD Dakar Senegal

The objectives of this study are to understand the mechanisms involved in the stabilization of water/oil interfaces by polymeric nanoparticles (NPs) (Eudragit®). Eudragit L100 NPs of various sizes and Zeta potentials were studied and compared at a water/cyclohexane model interface using a droplet tensiometer (Tracker Teclis, Longessaigne, France). The progressive interfacial adsorption of the NPs in the aqueous phase was monitored by tensiometry. The model interface was maintained and observed in a drop tensiometer, analyzed via axisymmetric drop shape analysis (ADSA), to determine the interfacial properties. Given the direct relationship between the stability of Pickering emulsions (emulsions stabilized by solid nanoparticles) and the interfacial properties of these layers, different nanoparticle systems were compared. Specifically, Eudragit NPs of different sizes were examined. Moreover, the reduction of the Zeta potential with PEG-6000 induces partial aggregation of the NPs (referred to as NP flocs), significantly impacting the stability of the interfacial layer. Dynamic surface tension measurements indicate a significant decrease in interfacial tension with Eudragit® nanoparticles (NPs). This reduction correlates with the size of the NPs, highlighting that this parameter does not operate in isolation. Other factors, such as the contact angle and wettability of the nanoparticles, also play a critical role. Notably, larger NPs further diminished the interfacial tension. This study enhances our understanding of the stability of Pickering emulsions stabilized by Eudragit® L100 polymeric nanoparticles.

关键词： Nanoparticles Eudragit® PEG Interfacial Tension Pickering Emulsion

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Phytochemical analysis and biological activities of Hertia cheirifolia L. roots extracts

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Asian Pacific Journal of Tropical Medicine 2017年第12期10卷 1134-1139页

作者： Kaouther Majouli Assia Hamdi Malek Besbes Hlila laboratory of Biochemistry Research Unit:UR 12ES08 “Cell Signaling and Pathologies”Faculty of MedicineUniversity of MonastirTunisia laboratory of Chemical Galenic and Pharmacological Development of DrugsFaculty of PharmacyUniversity of MonastirTunisia laboratory of Transmissible Diseases and of Biologically Active Substances MDT01Faculty of PharmacyUniversity of MonastirTunisia

Objective: To test the antioxidant, antimicrobial and a-glucosidase inhibitory activities of the roots extracts from Hertia cheirifolia(H. cheirifolia) ***: Total phenolics and total flavonoids content of the different extracts were determined by colorimetric methods and reverse phase high-performance liquid chromatography(RP-HPLC) was performed to identify various chemical *** different extracts were evaluated for antioxidant activities by 2,2-diphenyl-1-picrylhydrazyl(DPPH), 2,2-azino-bis-3-ethylenebenzothiozoline-6-sulfonic acid(ABTS·^+) and β-carotene bleaching tests and α-glucosidase inhibitory properties. The antimicrobial activity was carried out in vitro by the broth dilution ***: Trans-cinnamic acid, rutin hydrate, naringin and quercetin were the main compounds of the ethyl acetate extract from H. cheirifolia L. This extract has significant scavenging activity to decrease free radicals especially for DPPH and ABTS radicals. As well as, the ethyl acetate extract exhibited an antimicrobial property against bacterial strains. Bacillus licheniformis and Salmonella enterica were the most sensitive strains with minimum inhibitory concentration values of 0.156 mg/***: The ethyl acetate extract was found to be selectively antioxidant and antimicrobial.

关键词： Hertia cheirifolia Phytochemical analysis Antioxidant Antimicrobial α-Glucosidase inhibitory

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Antioxidant and Antibacterial Properties of <i>Mesembryanthemum crystallinum</i>and <i>Carpobrotus edulis</i>Extracts

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Advances in Chemical Engineering and Science 2012年第3期2卷 359-365页

作者： Bouftira Ibtissem Chedly Abdelly Souad Sfar laboratory of galenic pharmacy Faculty of Pharmacy Monastir Monastir Tunisia laboratory of Plant Adaptation to Abiotic Sresses CBBC Tunisia Tunisia

The two halophyte plants Mesembryanthemum crystallinum and Carpobrotus edulis (Family: Aizoaceae, Order: Cary-ophyllales), widely used in the traditional medicine, were chosen for this study. There is no much information about the antioxidant and antibacterial activities of the two plants growing in the Tunisian coasts. The most of studies conducted confirmed the responses of these plants to the abiotic stresses. We demonstrate a high antioxidant activity in the two plant extracts by using the 1,1-diphenyl-2-picrylhydrazyl (DPPH) method. The two plant extract also exhibited antibacterial activity by using the minimal inhibitory concentration (MIC) against bacterial strains;Escherichia coli (ATCC 25922), Pseudomonas aeruginosa (ATCC 27853) and Staphylococcus aureus (ATCC 25923). The different medicinal properties can be attributed in part to the presence of polyphenolics compounds in the two plant extracts.

关键词： Antibacterial Antioxidant Halophyte plants Flavonoids

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Preliminary Study on Counterfeiting of Artemether and Artesunate Marketed in Lubumbashi

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Pharmacology & pharmacy 2016年第5期7卷 185-192页

作者： Pierrot Mwamba Tshilumba Elie Rongorongo Kagoha Valentin Bashige Chiribagula Glauber Mbayo Kalubandika Vianney Ntabaza Ndage Trésor Sumbu Nzuzi Evodie Numbi Wa Ilunga Pierre Duez Jean Baptiste Kalonji Ndoumba laboratory of galenic pharmacy and Drug Analysis University of Lubumbashi Lubumbashi Democratic Republic of Congo laboratory of Therapeutic Chemistry and Pharmacognosy University of Mons Mons Belgium laboratory of Pharmacognosy University of Lubumbashi Lubumbashi Democratic Republic of Congo

Pharmaceutical counterfeiting is a health scourge responsible for several cases of morbidity and mortality. Counterfeit medicines cause therapeutic failure, emergence of resistance in the treatment of infections. This study was conducted in order to identify counterfeit and authentic medicines in circulation in Lubumbashi. The study included artemether and artesunate for oral administration. A careful visual inspection of medicine, investigation of authenticity of pharmaceutical products from manufacturers and pharmaceutical regulatory authorities and determination of content were used as study parameters. 52 samples: 37 artemether and 15 of artésunate were collected. 7 samples (13%) have proven to be counterfeit. Artemether was the most counterfeit (71%) and 29% for artesunate. 6 (12%) samples were substandard according to the international pharmacopoeia in terms of content of active ingredient. Sixty-seven percent of non-compliance concerned counterfeit medicines. The proportion of non-compliance is highest among counterfeit medicines (71.43% vs 2.22%;p = 0.000004). It is obvious that strengthening the capacity of the drug regulatory authority of the DRC reduces the influx of counterfeit drug and substandard.

关键词： Counterfeit Medicines Antimalarial Lubumbashi DR Congo

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Development and Validation of a Spectrofluorimetric Method for the Assay of Tetracycline in Capsules

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American Journal of Analytical Chemistry 2018年第3期9卷 162-170页

作者： Lucien Murhula Namegabe Serigne Omar Sarr Yérim Mbagnick Diop Department of galenic pharmacy Official University of Bukavu Bukavu Democratic Republic of the Congo Analytical Chemistry and Food Sciences laboratory Cheikh Anta Diop University Dakar Senegal National Medecines Control laboratory Dakar Senegal

The purpose of this study is to develop and validate a method for the analysis of tetracycline capsules by spectrofluorimetry. A pH 9 borate buffer was used as diluent of tetracycline after reaction with magnesium salt at the excitation wavelength of 372 nm and 516 nm of emission. A linear response was observed between 0.25 μg/mL and 1.5 μg/mL with a correlation coefficient (R) of 0.9998. The detection and quantification limits found are 0.0125 μg/mL and 0.0412 μg/mL respectively. The proposed method proved trueness with a recovery between 99.88% and 101.10%. The relative standard deviations of repeatability and intermediate precision found ≤2.88% reflected a good precision of the method. The proposed method is therefore valid within the limits of 90% to 110%. The proposed method was applied to the quality control of 9 tetracycline samples from market and gave results in accordance with the pharmacopoeia standards.

关键词： Validation Spectrofluorimetry Tetracycline

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Multiple Emulsions Able to Be Used for Oral Administration of Active Pharmaceutical Ingredients: Physico-Chemical Parameters Study of Different Phases

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Journal of Modern Physics 2020年第10期11卷 1528-1535页

作者： Louis Augustin Diaga Diouf Alphonse Rodrigue Djiboune Mamadou Soumboundou Sidy Mouhamed Dieng Papa Mady Sy Gora Mbaye Mounibé Diarra Pharmaceutical Physics and Biophysics laboratory Faculty of Medicine Pharmacy and Odontology Cheikh Anta Diop University of Dakar Dakar Senegal Pharmaceutical Physics and Biophysics laboratory Healthy UFR of Thies University of Thies Thies Senegal galenic and Industrial pharmacy laboratory Healthy UFR of Thies University of Thies Thies Senegal

Multiple emulsions are of great therapeutic interest especially in the administration of medicines which can be inactivated by digestive enzymes;moreover the researches of formulation not being often easy, a control of the different phases physicochemical parameters would be of great interest in rapid formulations and at low cost. When formulating emulsions, the preliminary tests, also known as formulation tests, constitute a step which can be long and expensive because of the quantity of reagents that can be used. A rigorous methodology could thus be of great interest, which is at the aim of our study which consists of evaluating the physico-chemical parameters of different phases used to make thus multiple emulsions. In our study, physico-chemical parameters such as conductivity, pH, density, viscosity, and surface tension have been studied by direct measurement using equipment and also by means of suitable mounting. The results showed that the pH and the surface tension have an important role in the prediction of the stability of emulsions, these latter must be of the same order of magnitude. For all phases conductivity does not have too much interest apart from helping to determine the type of the emulsion.

关键词： Active Pharmaceutical Ingredients Multiple Emulsions Stability Physico-Chemical Parameters

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Investigation of the Quality of Antibiotics-Based Amoxicillin for Monitoring of Some Different Medicine Markets of Democratic Republic of Congo

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American Journal of Analytical Chemistry 2018年第8期9卷 366-385页

作者： Nicodème Kalenda Tshilombo Patient Ciza Hamuli Jérémie K. Mbinze Védaste Habyalimana Dibungi T. Kalenda Don Jethro Mavungu Pierrot Mwamba Philippe Hubert Roland Djang’eing’a Marini laboratory of Analytical Chemistry CIRM Department of Pharmacy Liege University Liège Belgium laboratory of Chromatography Faculty of Pharmaceutical Sciences University of Kinshasa Kinshasa Democratic Republic of Congo laboratory of Drug Analysis Department of Galenic Pharmacy University of Kinshasa Kinshasa Democratic Republic of Congo Medical Procurement and Production Division Rwanda Biomedical Center Kigali Rwanda laboratory of Pharmacognosy CIRM Department of Pharmacy Liege University Liège Belgium Ecole Régionale Postuniversitaire d’Aménagement et de Gestion Intégrée des Forêts et Territoires Tropicaux University of Kinshasa Kinshasa Democratic Republic of Congo Department of pharmacy galenic University of Lubumbashi Lubumbashi Democratic Republic of Congo

In order to combat the counterfeiting of drugs, adapted HPLC analytical USP methods were applied to evaluate the quality of the amoxicillin (with or without potassium clavulanate) powder for suspension sold in some Congolese markets. The adaptation has been done by modifying the column dimensions and adjusting the flow rate. According to the intended deployment of these methods in Democratic Republic of Congo (DRC), 3 factors (analyst, day and equipment) were involved in the validation step while applying the classic total error measurement approach with an accuracy profile as decision tool. Since adequate results were obtained in terms of selectivity, precision, trueness and accuracy (tolerance limits of life expectancy: ?6.0% and 3.8%) for levels of interest concentration, the methods have been considered for routine use on several samples from different provenances and collected in 4 major DRC cities. Out of 278 samples collected, 200 were eligible for analysis from which 28% were found under standards with several figures: pH failure, out of specification for amoxicillin content, absence of potassium clavulanate, physical modifications of the powders. As evidenced by these findings, medicines of low-quality continue to be a major public health problem requiring appropriate action to effectively address this problem.

关键词： Poor Quality Medicines Amoxicillin LC Method Validation Survey Study

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Substandard/Falsification Antibacterial Agents: A Systematic Review of Liquid Chromatographic and Spectrophotometric Methods for Their Detection

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American Journal of Analytical Chemistry 2019年第8期10卷 348-365页

作者： Pierrot Mwamba Tshilumba Moke Muindu Mutshitshi Kasongo Gaelle Kalonji Mujinga Mbedi Zabakani Joel Kabadi Kasongo Musumba Tshamba Jean-Claude Nkwanga Roland Marini Djang’eing’a Pierre Duez Jean-Baptiste Kalonji Ndoumba laboratory of Drug Analysis and galenic University of Lubumbashi Lubumbashi Democratic Republic of Congo laboratory of Therapeutic Chemistry and Pharmacognosy University of Mons Mons Belgium Departement of Pharmacology and Toxicology University of Lubumbashi Lubumbashi Democratic Republic of Congo laboratory of Analytical Chemistry CIRM Department of Pharmacy Liege University Liège Belgium

Falsified antibacterial agents continue to pose serious public health problems around the world. They are notably responsible for resistance emergence in the treatment of infectious diseases that can lead to death. The aim of this study was to summarize the literature on the methods developed and validated to detect poor quality antibacterial agents in order to assess the impact of these available methods in the fighting against Counterfeit/substandard medicines. Thus, studies published in the time from January 2000 to July 2017, were accessible via Google Scholar and Pubmed and allowed to analyze 41 papers. The majority (30) of developed and validated methods concerned LC methods, 9 regarded UV/V is spectrophotometry and two studies simultaneously developed both methods. Antibacterial agents belonging to beta-lactams group were the most concerned by the methods developed and validated (39%), followed by quinolones (18%) and macrolides (12%). Regarding active ingredients, amoxicillin (12%) was the most concerned by the development and validation methods. In spite of several available methods to detect substandard drugs, antibacterial agents for which methods were developed and validated were the most concerned by worldwide detected non-conformities. The fight against this scourge should not be only limited by their detection, but it also requires an effective involvement of different actors notably: health authorities, international organizations, pharmaceutical industries etc.

关键词： Counterfeiting/Falsification/Substandard Antibacterial Liquid Chromatography/Spectrophotometry UV/Vis

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Quality Control of Quinine in Pharmaceutical Forms Tablets Find East of the Democratic Republic of Congo

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American Journal of Analytical Chemistry 2019年第9期10卷 415-422页

作者： Lucien Murhula Namegabe Mireille Tumusifu Kadhesi Pacifique Murhula Hamuli Aladdin Ombeni Mahano Paul Brioen Department of galenic pharmacy Official University of Bukavu Bukavu DRC Analytical Chemistry and Food Sciences laboratory Official University of Bukavu Bukavu DRC Medicinal Plant Research and Drug Development at PAU-UI University of Ibadan Ibadan Nigeria Faculty of Medicine and pharmacy Official University of Bukavu Bukavu DRC

The present study focuses on the quality control of quinine in the compressed pharmaceutical forms circulating in eastern Democratic Republic of Congo. The analyses performed on the collected samples included disintegration of the tablets, identification of quinine in the formulations by color reaction methods and thin-layer chromatography. The quantitative analysis was performed by spectrophotometric and volumetric methods. The most significantly observed findings were abnormalities of release;underdosing, overdosing and absence of the active ingredient, Which brings us to the conclusion that more than 30% of the samples analyzed are of inferior quality and adulterated.

关键词： Quality-Control Quinine Tablets

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Quality Control of Tramadol in Kisangani: Development, Validation, and Application of a UV-Vis Spectroscopic Method

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American Journal of Analytical Chemistry 2021年第8期12卷 295-309页

作者： Marguerite Borive Amani Jérémie Mbinze Kindenge Emile Tweni Baruti Elodie Nsasi Bakiantima Salomon Batina Agasa Philippe Hubert Roland Marini Djang’eing’a Department of pharmacy Faculty of Medicine and Pharmacy University of Kisangani Kisangani Democratic Republic of the Congo laboratory of Drugs Analysis Department of Galenic and Drug Analysis Faculty of Pharmaceutical Sciences University of Kinshasa Kinshasa Democratic Republic of the Congo Department of Internal Medicine Faculty of Medicine and Pharmacy University of Kisangani Kinshasa Democratic Republic of the Congo laboratory of Analytical Pharmaceutical Chemistry Faculty of Medicine University of Liège Liège Belgium

Context: Substandard and falsified medicines are circulating in low-income countries mostly without any control. We availed a simple and not expensive UV-Vis spectroscopic method to evaluate the quality of tramadol in Kisangani before and during the Covid-19 period. Methods: For the analytical quantitative method, an experimental design was applied to set up the optimal levels of the selected factors, namely, pH of dissolution medium, type of cuvette, and wavelength. Taking into account the capsule pharmaceutical formulation within 80 - 120 μg·mL-1 concentration range, we analyzed 89 tramadol samples from pharmacies and hospitals of the six Kisangani municipalities. Results: pH showed a significant effect on absorbance, whereas quartz cuvette and wavelength did not. A typical 100 μg·mL-1 tramadol solution gave an absorbance of 0.64 at 272 nm. Validation highlighted a matrix effect observed with a 6% bias. A correction factor of 0.9372 allowed to improve the accuracy profile, which were then totally included within the 10% acceptance limits. Quality control revealed that 25 samples out of 89 were not compliant in terms of manufacturing license, registration status in DRC and content as well. Conclusion: This study showed that the strengthening of analytical strategy in Kisangani is a need.

关键词： Tramadol UV-Vis Spectroscopy Method Development Validation Quality Control

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