Current Issue : July - September Volume : 2020 Issue Number : 3 Articles : 5 Articles
Taro Boloso-I (TB1), a newly improved Colocasia esculenta variety, is a potential source of starch with high yield. However, to\nimprove some limitations of the native starches (NS), such as flowability and compactibility, different physical and chemical starch\nmodifications have been employed. Acetylation is one of the chemical modifications which improves the flow and compaction of the\nNS, which are prerequisite during direct compression (DC) of tablets. Hence, in this study, TB1 starch was acetylated using acetic\nanhydride and evaluated as an ideal excipient for direct compression. Starch acetates (SA) with a degree of substitution (DS) of 0.072\n(SA1) and 0.695 (SA2) were produced and evaluated. FTIR spectra of the SAs were used to verify the acetylation of the NS. Powder\nflow evaluation parameters showed significant improvement in the flow properties of the NS following acetylation. In addition, the\nswelling power, solubility, and compactibility were also improved. Tensile strength (TS) of the tablets comprising SAs only, SA1\n(41.40) and SA2 (63.43 Kg/cm2), was significantly higher than tablets made of the NS (31.96) and Starch 1500® (15.12 Kg/cm2). The SAs\nalso showed lower sensitivity towards lubrication than the NS and Starch 1500® as lower lubricant sensitivity ratios were recorded. In\naddition, tablets comprising the SAs satisfactorily accommodated at least up to 50% w/w paracetamol-compared to 30 %w/w by Starch\n1500®-upon DC processing. The paracetamol tablets comprising SAs also complied with the United States Pharmacopeia specifications\nfor disintegration and dissolution studies. Therefore, taking all the facts into consideration, the SAs could be potential DC excipients in\ntablet formulations....
Abstract: Ellagic acid (EA) is a potent antioxidant substance of natural origin characterized by poor\nbiopharmaceutical properties and low solubility in water that limit its use. The aim of the present\nstudy was to develop lipid-based nanoparticle formulations able to encapsulate EA for dermal\ndelivery. The EA-loaded nanoparticles were prepared using two different lipid compositions, namely\ntristearin/tricaprylin (NLC-EA1) and tristearin/labrasol (NLC-EA2). The influence of formulations on\nsize, entrapment efficiency, and stability of EA-loaded nanoparticles was investigated. Cryo-TEM and\nsmall-angle X-ray scattering (SAXS) analyses showed that no morphological differences are evident\namong all the types of loaded and unloaded nanostructured lipid carriers (NLCs). The macroscopic\naspect of both NLC-EA1 and NLC-EA2 did not change with time. No difference in size was\nappreciable between empty and drug-containing NLC, thus the nanoparticle diameter was not\naffected by the presence of EA and in general no variations of the diameters occurred during this time.\nThe entrapment efficiency of both EA-loaded nanoparticles was almost quantitative. In addition,\nNLC-EA1 maintained EA stability for almost two months, while NLC-EA2 up to 40 days. FRAP (Ferric\nreducing ability of plasma) assay showed an antioxidant activity around 60% for both the loaded\nNLC, as compared to the solution. Although both types of NLC are characterized by some toxicity on\nHaCaT cells, NLC-EA1 are less cytotoxic than NLC-EA2. Taken together these results demonstrated\nthat the inclusion of EA within NLC could improve the water solubility, allowing for a reduction of\nthe dosage. Moreover, both types of NLC-EA maintained a high antioxidant effect and low toxicity....
Ethiopian potato is one of the tuber-bearing members of the family Lamiaceae. It is an indigenous crop in Ethiopia and important\nsource of starch. Unprocessed native starches are structurally weak and functionally restricted for application in pharmaceutical\ntechnologies. Consequently, starch is usually modified either chemically or physically to make it convenient for industrial use.\nThe aim of the study was to prepare and characterize acid-modified Ethiopian potato starch (AMEPS) and evaluate its\nfunctionality as a direct compressible excipient in tablet formulations. The extracted starch from Ethiopian potato tuber was\nmodified using 6% HCl concentration for 8 days, then dried using oven and spray drying techniques, and subsequently\nevaluated and compared with the native Ethiopian potato starch (NEPS) and S1500® as a direct compressible excipient. Acid\nmodification of the NEPS decreased the moisture content and swelling power while increased the percent solubility. The X-ray\ndiffraction revealed that both the NEPS and AMEPS have B-type crystal patterns. The AMEPS showed improved flowability\ncompared to the NEPS. This improvement was further enhanced by the spray drying process. The compactability study revealed\nthat the tensile strength of spray-dried AMEPS (16.76 kg/cm2) was significantly higher than that of the spray-dried NEPS\n(7.07 kg/cm2) and S1500® (11.66 kg/cm2). The AMEPS was less sensitive to lubricants compared to the NEPS and Starch 1500®.\nSimilarly, the dilution potential of the AMEPS was superior to the NEPS and S1500®. The AMEPS accommodated up to 50% of\nparacetamol while the NEPS and S1500® were able to hold only up to 30%. Pharmacopoeial specifications for disintegration and\ndissolution were met by the paracetamol tablets prepared by AMEPS. Thus, considering all the results obtained, spray-dried\nAMEPS could be a potential alternative directly compressible tablet excipient....
Eosinophilic esophagitis (EE) is a chronic immune/antigen-mediated esophageal\ninflammatory disease for which off-label topical corticosteroids (e.g., budesonide) are widely used in\nclinic. In general, thickening excipients are mixed with industrial products to improve the residence\ntime of the drug on the esophageal mucosa. The compounding procedures are empirical and the\ncomposition is not supported by real physicochemical and technological characterization. The\ncurrent study aimed to propose a standardized budesonide oral formulation intended to improve\nthe resistance time of the drug on the esophageal mucosa for EE treatment. Different placebo\nand drug-loaded (0.025% w/w) formulations were prepared by changing the percentage of xanthan\ngum alone or in ratio 1:1 with guar gum. Both excipients were added in the composition for their\nmucoadhesive properties. The formulative space was rationalized based on the drug physicochemical\nstability and the main critical quality attributes of the formulation, e.g., rheological properties,\nsyringeability, mucoadhesiveness and in vitro penetration of budesonide in porcine esophageal\ntissue. The obtained results demonstrated that gums allowed a prolonged residence time. However,\nthe concentration of the mucoadhesive polymer has to be rationalized appropriately to permit the\nsyringeability of the formulation and, therefore, easy dosing by the patient/caregiver....
Background: Drug-coated balloons (DCBs), which deliver anti-proliferative drugs with\nthe aid of excipients, have emerged as a new endovascular therapy for the treatment of peripheral\narterial disease. In this study, we evaluated the use of keratose (KOS) as a novel DCB-coating\nexcipient to deliver and retain paclitaxel. Methods: A custom coating method was developed to\ndeposit KOS and paclitaxel on uncoated angioplasty balloons. The retention of the KOS-paclitaxel\ncoating, in comparison to a commercially available DCB, was evaluated using a novel vascular-motion\nsimulating ex vivoflowmodel at 1 h and 3 days. Additionally, the locoregional biological response of the\nKOS-paclitaxel coating was evaluated in a rabbit ilio-femoral injury model at 14 days. Results: The KOS\ncoating exhibited greater retention of the paclitaxel at 3 days under pulsatile conditions with vascular\nmotion as compared to the commercially available DCB (14.89...............
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