Current Issue : July - September Volume : 2019 Issue Number : 3 Articles : 6 Articles
The family of graphene has attracted increasing attention on account of their large specific surface area and good mechanical\nproperties in the biomedical field. However, some characteristics like targeted delivery property and drug delivery capacity could\nnot satisfy the need of a drug carrier. Herein, a graphene oxide (GO) nanocarrier was designed by modification of a folic acid\n(FA) derivative..........................
Paliperidone is a well known dopamine antagonist of the atypical antipsychotic class. In present study paliperidone was formulated as matrix type sustained release tablets using natural polymers. Gum exudates are among the oldest natural polymers. They are already being used as thickening and stabilizing agent from last several years. The plant derived polymers comply with many requirements of pharmaceutical excipients. The aim of sustained release formulation is to reduce the frequency of dosing. Tablets were prepared by direct compression method. The optimized formulations contain paliperidone as active ingredient and guar gum, xanthum gum and Acacia gum are used as polymers. The evaluation parameters include the thickness, weight variation test, drug content, hardness, friability and in-vitro release studies. Based on the results of in-vitro studies it was concluded that the natural polymers can be used as an efficient matrix former to provide sustained release of paliperidone. The release of paliperidone was prolonged for 20 hrs, indicating the usefulness of the formulations for once daily dosage forms. Thus the reducing frequency of dosing increases patient compliance....
Based on the formation of carbodiimide compounds between carboxyl and primary amines, hollow microspheres arising fromthe\nfolic acid (folate-FA) grafted onto the surface of the modified hydroxyapatite were successfully prepared.The hollow morphology\nand composition of the FA-grafted hydroxyapatitemicrosphereswere confirmed by scanning electronmicroscopy (SEM) and other\ncharacterizations. Brunauer-Emmett-Teller (BET) assay revealed the specific surface area and average pore size of the microspheres\nwere 34.58m^2/g and 17.80 nm, respectively. As a drug carrier, the kinetic investigation of doxorubicin (DOX) loaded shows that the\nadsorbed behavior of drug on the adsorbent is more suitable to be described with pseudo-first-order model. Furthermore, the\nrelease rate can reach 83% at pH 5.7, which is greater than the release of 39% at pH 7.4, indicating an excellent performance of\ncontrolled drug release for response pH. The releasemechanismof DOX coincides with Fickian diffusion as a result of Korsmeyer-\nPeppas model analysis and the release phenomena can be well explained by Fickian diffusion second law....
Traditional approaches to achieve sustained delivery of pharmaceutical peptides\ntraditionally use co-excipients (e.g., microspheres and hydrogels). Here, we investigate the release of\nan amyloidogenic glucagon analogue (3474) from an aggregated state and the influence of surfactants\non this process. The formulation of peptide 3474 in dodecyl maltoside (DDM), rhamnolipid (RL), and\nsophorolipid (SL) led to faster fibrillation. When the aggregates were subjected to multiple cycles\nof release by repeated resuspension in fresh buffer, the kinetics of the release of soluble peptide\n3474 from different surfactant aggregates all followed a simple exponential decay fit, with half-lives\nof 5-18 min and relatively constant levels of release in each cycle. However, different amounts\nof peptide are released from different aggregates, ranging from 0.015 mg/mL (3475-buffer) up to\n0.03 mg/mL (3474-DDM), with 3474-buffer and 3474-RL in between. In addition to higher release\nlevels, 3474-DDM aggregates showed a different amyloid FTIR structure, compared to 3474-RL\nand 3474-SL aggregates and a faster rate of degradation by proteinase K. This demonstrates that\nthe stability of organized peptide aggregates can be modulated to achieve differences in release of\nsoluble peptides, thus coupling aggregate polymorphism to differential release profiles. We achieved\naggregate polymorphism by the addition of different surfactants, but polymorphism may also be\nreached through other approaches, including different excipients as well as changes in pH and\nsalinity, providing a versatile handle to control release profiles....
Omega-3 fatty acid plays a role in protecting cells in the human body, maintaining the\nstructure of the cell, and helping smooth metabolism. Also, it inhibits the formation of blood clotting\nand is effective in enhancing the formation of bone. However, the instability due to fatty acid\noxidation and a fishy smell are the reasons it is avoided by people. In this study, we tried to obtain\nthe omega-3 powder through spray-drying method using a variety of binders and surfactants for\nimproving the limit of omega-3 fatty acid. First of all, an olive oil was used instead of omega-3 for\noptimization of the preparation of spray-dried omega-3 powder....................
Hydroquinone (HQ) is an anti-hyperpigmentation agent with poor physicochemical\nstability. HQ formulations are currently elaborated by compounding in local pharmacies.\nVariability in the characteristics of HQ topical formulations can lead to remarkable differences in\nterms of their stability, efficacy, and toxicity. Four different semisolid O/W formulations with 5%\nHQ were prepared using: i) Beeler´s base plus antioxidants (F1), ii) Beeler´s base and dimethyl\nisosorbide (DMI) as solubiliser (F2), iii) olive oil and DMI (F3), and iv) Nourivan®, a skinmoisturising\nand antioxidant base, along with DMI (F4). Amongst the four formulations, F3 showed\nthe greatest physicochemical stability with less tendency to coalescence but with marked chromatic\naberrations. An inverse correlation was established by multivariate analysis between the mean\ndroplet size in volume and the steady-state flux, which explains why F3, with the smallest droplet\nsize and the most hydrophobic excipients, exhibited the highest permeation across both types of\nmembranes with enhancement ratios of 2.26 and 5.67-fold across Strat-M® and mouse skin,\nrespectively, compared to F1. It is crucial to understand how the HQ is formulated, bearing in mind\nthat the use of different excipients can tune the transdermal delivery of HQ significantly....
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