10 research outputs found

    Mikrosfere s mukuna gumom za peroralnu primjenu glibenklamida: In vitro ispitivanje

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    An investigation into the suitability of mucuna gum microspheres for oral delivery of glibenclamide is presented. Mucuna gum microspheres were formulated under different conditions of polymer concentration and crosslinking time at constant speed. The formulated microspheres were thereafter loaded with glibenclamide by the remote loading process. The microspheres were evaluated according to particle size, yield, loading efficiency and swelling. In vitro release of glibenclamide from the microspheres was studied in simulated intestinal fluid (SIF, pH 7.4). The release data was fitted into two release models to investigate the mechanism of glibenclamide release from the microspheres. All the microspheres showed good swelling characteristics in distilled water. The investigation revealed that the microspheres produced with 5% (m/V) mucuna gum with a crosslinking time of 5 h had the optimum prolonged release pattern. The microspheres produced using 10% (m/V) mucuna gum with a crosslinking time of 1 h had the highest delayed release of the incorporated drug whereas those without crosslinking had the fastest release of the incorporated active ingredient. Ritger-Peppas case I transport model appeared to have adequately described the release process as about 54% of the batches of microspheres conformed to this model. This implies that a formulation of glibenclamide-loaded mucuna gum microspheres is likely to offer a reliable means of delivering glibenclamide by the oral route.U radu je opisana priprava mikrosfera s mukuna gumom za peroralnu primjenu glibenklamida. Pri izradi mikrosfera varirana je koncentracija polimera i vrijeme umre┼żavanja, a brzina je bila konstantna. Mikrosfere su zatim punjene glibenklamidom metodom odvojenog punjenja. Pripravljenim mikrosferama procijenjena je veli─Źina ─Źestica, iskori┼ítenje, u─Źinkovitost punjenja (LE %) i sposobnost bubrenja. In vitro osloba─Ĺanje glibenklamida iz mikrosfera pra─çeno je u simuliranoj intestinalnoj teku─çini (SIF, pH 7.4). Za odre─Ĺivanje mehanizma osloba─Ĺanja ispitana su dva modela. Sve mikrosfere su imale dobru sposobnost bubrenja u destiliranoj vodi. Optimalno produljeno osloba─Ĺanje glibenklamida postignuto je iz mikrosfera prire─Ĺenih s 5% (m/V) mukuna gume, uz vrijeme umre┼żavanja 5 h. Ljekovita tvar se najsporije osloba─Ĺala iz mikrosfera prire─Ĺenih s 10% (m/V) mukuna gume, uz vrijeme umre┼żavanja 1 h, dok se najbr┼że osloba─Ĺala iz mikrosfera s 10% (m/V) gume, bez umre┼żavanja. Nekoliko mehanizama osloba─Ĺanja uklju─Źeno je u otpu┼ítanje ljekovite tvari iz mikrosfera. Me─Ĺutim, Ritger-Peppasov transportni model I opisuje proces osloba─Ĺanja u 54% slu─Źajeva, ┼íto zna─Źi da mikrosfere glibenklamida s mukuna gumom predstavljaju pouzdan sustav za peroralnu primjenu te ljekovite tvari

    Antimicrobial activity of Psidium guajava Linn. stem extracts against methicillin-resistant Staphylococcus aureus

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    The antimicrobial activities of the water and methanolic extracts of Psidium guajava Linn. stem bark were evaluated against eight methicillin-resistant Staphylococcus aureus (MRSA) isolates. The plant material was extracted and phytochemical analyses were performed by standard procedures. The agar diffusion method was employed for the assessment of the sensitivity of the extracts, while the agar dilution technique was employed for the quantitative determination of the bacteriostatic and bacteriocidal activities of the plant extracts. The phytochemical studies of P. guajava revealed the presence of carbohydrates, glycosides, tannins, and proteins as its major constituents. Results show that the methanolic and water extracts of P. guajava stem bark exhibited antibacterial activity against methicillin resistant S. aureus bacteria. The minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) of the stem bark water extracts ranged from 125 to 500 ┬Ág/ml while that of the stem bark methanol extract ranged from 62.5 to 250 ┬Ág/ml.Key words: Psidium guajava, antimicrobial activity, phytochemical screening, methillin-resistant┬á staphylococcus aureus

    Recent advances in particulate anti-malarial drug delivery systems: A review

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    Malaria remains a tremendous health burden in tropical areas, causing a life-threatening disease and accounts for 1 to 2 million deaths round the globe yearly. Researchers have explored different novel approaches to deliver and improve the biopharmaceutical performance of drugs used in malaria chemotherapy. These novel drug delivery systems (NDDS) enhanced bioavailability of these drugs and also may offer controlled release of these drugs. The major aim of the NDDS is to improve the efficacy of these drugs, and at the same time to eliminate their toxicity. These NDDS include: micro/nanoparticulate DDS, emulsion based DDS, dendrimers and liposomes among others. The development of these particulate carriers as vehicles for the delivery of active compounds is a novel area of research that provides a new hope in malarial chemotherapy. The work presents various trends in malarial chemotherapy, as well as an exhaustive screening of different particulate drug delivery systems (PDDS) and the recent advances in the delivery of anti-malarial drugs using the novel particulate drug delivery systems (NPDDS)

    Preliminary spectroscopic characterization of PEGylated mucin, a novel polymeric drug delivery system

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    The objective of this study was to evaluate, spectrophotometrically, the compatibility of non-mucinated polyethylene glycol (PEG) 4000 and non-PEGylated mucin in a PEGylated mucin matrices for drug delivery application. Mucin was extracted from the giant African land snails (Archachatina maginata) using chilled acetone and characterized in terms of qualitative properties and solubility profile. Polymeric matrices composed of PEG 4000 and mucin in ratios of 2:0 (A), 1:1 (B), 2:1(C) and 3:1 (D) were prepared by co-precipitation using chilled acetone. The matrices were characterized with respect to compatibility using the Fourier transform infrared (FT-IR) spectroscopy. Results of the qualitative tests performed on the snail mucin showed that carbohydrates, proteins and trace amounts of fats were present; the extracted mucin was light-brownish in colour, with a pleasant meaty odour. Snail mucin, when dispersed in water yielded a slightly viscous dispersion, but is not soluble in ethanol, acetone, 0.1 M sodium hydroxide, ammonium hydroxide and sulphuric acid. The presence of different peaks in the FT-IR spectra of the PEGylated mucin matrices compared with the non-PEGylated mucin (2:0) matrix and non-mucinated PEG 4000 (0:2) matrix indicated the formation of new polymers, which could be employed in drug delivery. This study has shown that PEGylation of mucin gives rise to new polymeric system with principal FT-IR peaks quite different from those of non-PEGylated mucin and nonmucinated PEG, and this may be employed in the delivery of drugs.Key words: PEGylation, drug delivery, mucin, Fourier transform infrared (FT-IR) spectroscopy, Archachatina maginata

    Improved antimalarial activity of caprol-based nanostructured lipid carriers encapsulating artemether-lumefantrine for oral administration

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    Background: Artemether and lumefantrine display low aqueous solubility leading to poor release profile; hence the need for the use of lipid-based systems to improve their oral bioavailability so as to improve their therapeutic efficacy. Aim and objective: The objective of this work was to utilize potentials of nanostructured lipid carriers (NLCs) for improvement of the oral bioavailability of artemether and lumefantrine combination and to evaluate its efficacy in the treatment of malaria. This study reports a method of formulation, characterization and evaluation of the therapeutic efficacies of caprol-based NLC delivery systems with artemether and lumefantrine. Method: The artemether-lumefantrine co-loaded NLCs were prepared using the lipid matrix (5% w/w) (containing beeswax and Phospholipon\uae 90H and Caprol-PGE 860), artemether (0.1%w/w) and lumefantrine (0.6%w/w), sorbitol (4%w/w), Tween\uae 80( 2%w/w as surfactant) and distilled water (q.s to 100%) by high shear homogenization and evaluated for physicochemical performance. The in vivo antimalarial activities of the NLC were tested in chloroquine-sensitive strains of Plasmodium berghei (NK-65) using Peter\ub4s 4-day suppressive protocol in mice and compared with controls. Histopathological studies were also carried out on major organs implicated in malaria. Results: The NLC showed fairly polydispersed nano-sized formulation (z-average:188.6 nm; polydispersity index, PDI=0.462) with no major interaction occurring between the components while the in vivo study showed a gradual but sustained drug release from the NLC compared with that seen with chloroquine sulphate and Coartem\uae. Results of histopathological investigations also revealed more organ damage with the untreated groups than groups treated with the formulations. Conclusion: This study has shown the potential of caprol-based NLCs for significant improvement in oral bioavailability and hence antimalarial activity of poorly soluble artemether and lumefantrine. Importantly, this would improve patient compliance due to decrease in dosing frequency as a sustained release formulation

    Nanotechnology based drug delivery systems for the treatment of anterior segment eye diseases

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    Diseases affecting the anterior segment of the eye are the primary causes of vision impairment and blindness globally. Drug administration through the topical ocular route is widely accepted because of its user/patient friendliness - ease of administration and convenience. However, it remains a significant challenge to efficiently deliver drugs to the eye through this route because of various structural and physiological constraints that restrict the distribution of therapeutic molecules into the ocular tissues. The bioavailability of topically applied ocular medications such as eye drops is typically less than 5%. Developing novel delivery systems to increase the retention time on the ocular surfaces and permeation through the cornea is one of the approaches adopted to boost the bioavailability of topically administered medications. Drug delivery systems based on nanotechnology such as micelles, nanosuspensions, nanoparticles, nanoemulsions, liposomes, dendrimers, niosomes, cubosomes and nanowafers have been investigated as effective alternatives to conventional ocular delivery systems in treating diseases of the anterior segment of the eye. This review discussed different nanotechnology-based delivery systems that are currently investigated for treating and managing diseases affecting the anterior ocular tissues. We also looked at the challenges in translating these systems into clinical use and the prospects of nanocarriers as a vehicle for the delivery of phytoactive compounds to the anterior segment of the eye

    Microsoft Word - 01

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    ABSTRACT The use of traditional medicines and phytopharmaceuticals for treating various ailments dates back several centuries. The aim of the present review is based on relevant data on the different approaches to formulation of various natural compounds from ethnomedicinal plants. Attempts are also being made to enumerate the possible leads from traditional medicinal system for the treatment of diseases. We tried to provide the readers with the array of processes, which can be further worked upon in clinical studies. Finally, this paper puts forth issues that need to be addressed by researchers in the future with respect to standardization of phytopharmaceuticals

    Novel Intravaginal Drug Delivery System Based on Molecularly PEGylated Lipid Matrices for Improved Antifungal Activity of Miconazole Nitrate

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    The aim of this study was to investigate the potential of microparticles based on biocompatible phytolipids [Softisan┬« 154 (SF) (hydrogenated palm oil) and super-refined sunseed oil (SO)] and polyethylene glycol- (PEG-) 4000 to improve intravaginal delivery of miconazole nitrate (MN) for effective treatment of vulvovaginal candidiasis (VVC). Lipid matrices (LMs) consisting of rational blends of SF and SO with or without PEG-4000 were prepared by fusion and characterized and employed to formulate MN-loaded solid lipid microparticles (SLMs) by melt-homogenization. The SLMs were characterized for physicochemical properties, anticandidal activity, and stability. Spherical discrete microparticles with good physicochemical properties and mean diameters suitable for vaginal drug delivery were obtained. Formulations based on SO:SF (1:9) and containing highest concentrations of PEG-4000 (4 %w/w) and MN (3.0 %w/w) were stable and gave highest encapsulation efficiency (83.05ÔÇô87.75%) and inhibition zone diameter (25.87┬▒0.94ÔÇô26.33┬▒0.94 mm) and significantly (p<0.05) faster and more powerful fungicidal activity regarding killing rate constant values (7.10 x 10Ôłĺ3ÔÇô1.09 x 10Ôłĺ2 minÔłĺ1) than commercial topical solution of MN (Fungusol┬«) (8.00 x 10Ôłĺ3 minÔłĺ1) and pure MN sample (5.160 x 10Ôłĺ3 minÔłĺ1). This study has shown that MN-loaded SLMs based on molecularly PEGylated lipid matrices could provide a better option to deal with VVC

    Effect of molecular interaction on the antiplasmodial efficacy of lumefantrine in amorphous polymethacrylate-urea solid solution

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    Malaria, a leading cause of mortality and morbidity in the developing world, with children aged under 5 years, accounts for 61% of all the global malaria deaths. The World Health Organization approved fixed-dose first-line artemisinin-based combination therapy (ACT) ÔÇô artemether-lumefantrine for effective malaria treatment, is challenged by poor aqueous solubility and inadequate bioavailability leading to treatment failures and emergence of resistant strains. This study focuses on evaluating novel lumefantrine (LF) polymethacrylate-urea solid solutions comprising of a retarding polymer for enhanced anti-plasmodial efficacy comparable with existing artemether-lumefantrine combination therapy. Lumefantrine polymethacrylate-urea solid solutions were prepared by solvent evaporation and characterized by differential scanning calorimetry (DSC), and dissolution studies. In vivo anti-plasmodial activity was determined by measuring the schizonticidal activity of Plasmodium berghei-infected mice using the PeterÔÇÖs 4-day curative test and the safety of the solid solutions was tested in major organs implicated in malaria. The solid state characterizations confirmed the formation of amorphous lumefantrine polymethacrylate-urea solid solutions. There was greater drug release from the matrix polymer in acidic than basic biorelevant media, with release kinetics following the Higuchi order. Interestingly, the reduction in parasitaemia caused by the lumefantrine polymethacrylate-urea formulations (72.3 and 81.27 %) for ternary and quaternary systems, batches SDA3 and SDB3, respectively) were significantly higher (p &lt; 0.05) and more sustained than lumefantrine pure powder, but with comparable efficacy to the commercial brand-Coartem┬«. The formulation was stable over a period of 6 months. Thus, this study provides useful information on developing sustained lumefantrine formulation with improved solubility and antiplasmodial efficacy. Keywords: Solid dispersion, lumefantrine, solubility, parasitaemia reduction, eudragit polymer, Urea

    Quinine: Redesigned and Rerouted

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    Quinine hydrochloride (QHCl) has remained a very relevant antimalarial drug 400 years after its effectiveness was discovered. Unlike other antimalarials, the development of resistance to quinine has been slow. Hence, this drug is to date still used for the treatment of severe and cerebral malaria, for malaria treatment in all trimesters of pregnancy, and in combination with doxycycline against multidrug-resistant malaria parasites. The decline in its administration over the years is mainly associated with poor tolerability due to its gastrointestinal (GIT) side effects such as cinchonism, complex dosing regimen and bitter taste, all of which result in poor compliance. Hence, our research was aimed at redesigning quinine using nanotechnology and investigating an alternative route for its administration for the treatment of malaria. QHCl nanosuspension (QHCl-NS) for intranasal administration was prepared using lipid matrices made up of solidified reverse micellar solutions (SRMS) comprising Phospholipon┬« 90H and lipids (Softisan┬« 154 or Compritol┬«) in a 1:2 ratio, while Poloxamer┬« 188 (P188) and Tween┬« 80 (T80) were used as a stabilizer and a surfactant, respectively. The QHCl-NS formulated were in the nanosize range (68.60 ┬▒ 0.86 to 300.80 ┬▒ 10.11 nm), and highly stable during storage, though zeta potential was low (ÔëĄ6.95 ┬▒ 0.416). QHCl-NS achieved above 80% in┬ávitro drug release in 6 h. Ex┬ávivo permeation studies revealed that formulating QHCl as NS resulted in a 5-fold and 56-fold increase in the flux and permeation coefficient, respectively, thereby enhancing permeation through pig nasal mucosa better than plain drug solutions. This implies that the rate of absorption as well as ease of drug permeation through porcine nasal mucosa was impressively enhanced by formulating QHCl as NS. Most importantly, reduction in parasitaemia in mice infected with Plasmodium┬áberghei ANKA by QHCl-NS administered through the intranasal route (51.16%) was comparable to oral administration (52.12%). Therefore, redesigning QHCl as NS for intranasal administration has great potential to serve as a more tolerable option for the treatment of malaria in endemic areas
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