Fickian Release Research Articles

Experimental and Modelling Study of Controlled Release from Dextran-Based Cryogels.

In this work, five different dextran-based cryogels for controlled drug release are investigated. Vitamin B12 was used as a model drug for in vitro release tests. Two different drug-loading procedures were adopted, leading to very different drug release curves. Indeed, a fast Fickian release was observed when freeze-dried samples of DEX40PEG360MA and DEX40PEG500MA were infused with the drug after cryogel formation. On the contrary, a slowed highly non-Fickian behavior arises when the drug is loaded before the low-temperature crosslinking step, leading to the cryogel formation. The non-Fickian drug release, observed for all the five different dextran-based cryogels investigated, is actually due to the cryoconcentration phenomenon, modeled with a two-step release process. The proposed transport model accurately predicts experimental release curves characterized by a long lag time, confirming that dextran-based cryogels are suitable for controlled release.

In vitro release modeling of beta-carotene from Bene oleosome and electrosprayed Quince seed hydrocolloids loaded with oleosomes containing beta-carotene

This research aimed to extract oleosome from the Bene kernel as a carrier of beta-carotene (3, 5, and 10 % w/w) and then use oleosomes in the Quince seed gum (QSG) electrosprayed nanoparticles for the sustained release of beta-carotene in food simulant. Oleosomes loaded with 5 % w/w beta-carotene had the highest encapsulation efficiency (94.53 % ± 1.23 %) and were used at 1, 3, and 5 % w/w in the QSG electrosprayed nanoparticles. Electrospray feed solutions containing 5 % oleosomes loaded with beta-carotene had the highest zeta potential (−34.45 ± 0.58 mV) and the lowest surface tension (23.47 ± 1.10 mN/m). FESEM images showed that with the increase of oleosomes up to 3 % w/w, the average size of the electrosprayed particles decreases. The Fourier transform infrared (FTIR) test proved the presence of protein in the oleosomes and their successful extraction from Bene seeds. Differential scanning calorimetry (DSC) and FTIR proved the successful entrapment of beta-carotene in the oleosomes structure and the successful placement of oleosomes containing beta-carotene in the electrosprayed nanoparticles. The predominant driving force involving the release of beta-carotene from the designed structures in food simulants was the Fickian release mechanism. The Peleg model was introduced as the best model describing the beta-carotene release.

Potential Application of Ovalbumin Gel Nanoparticles Loaded with Carvacrol in the Preservation of Fresh Pork.

Plant essential oil has attracted much attention in delaying pork spoilage due to its safety, but its low antibacterial efficiency needs to be solved by encapsulation. Our previous research had fabricated a type of ovalbumin gel nanoparticles loaded with carvacrol (OCGn-2) using the gel-embedding method, which had a high encapsulation rate and antibacterial activity. The main purpose of this study was to further evaluate the stability and slow-release characteristics of OCGn-2 and potential quality effects of the nanoparticles on the preservation of fresh pork pieces during 4 °C storage. The particle test showed that the nanoparticles had better heat stability below 85 °C and salt stability below 90 mM. The in vitro release study indicated that the carvacrol in OCGn-2 followed a Fickian release mechanism. The pork preservation test suggested that the OCGn-2 coating treatments could remarkably restrict the quality decay of pork slices compared to free carvacrol or a physical mixture of ovalbumin and carvacrol treatment. Nano-encapsulation of ovalbumin is beneficial to the sustained release, enhanced oxidation resistance, and improved antibacterial activity of carvacrol. The study suggested that ovalbumin gel nanoparticles embedded with carvacrol could be applied as an efficient bacterial active packaging to extend the storage life of pork.

Formulation and Evaluation of Fast Disintegrating Tablets of Ondansetron Using Natural Superdisintegrants

Background: Fast disintegrating tablet (FDT) of ondansetron has better patient compliance as it is easy to swallow for the treatment of nausea and vomiting. Moreover, fast absorption, rapid onset, reduced loss of drugs, and enhanced bioavailability are making oral dispersible systems a better drug delivery system. This research was conducted with the objective to formulate and evaluate the oral FDT of ondansetron HCl using natural polymers. Methods: The tablets were formulated employing the direct compression technique using different ratios of natural super disintegrants such as spray-dried banana powder, ispaghula husk powder, and combination of both polymers. The developed powders were subjected to the pre-compression parameters and the powders were punched using a single-head rotatory compression machine. The formulated 200 mg tablets were subjected to post-compression evaluation. Results: The Fourier-transform infrared spectroscopy studies showed no chemical interaction between pure drugs, natural super disintegrants, and other excipients. Formulation F6 containing ispaghula husk powder in a 1:4 ratio demonstrated 98.60±0.003% of drug release within 10 minutes indicating the best formulation. Conclusion: FDT of ondansetron was considered the best formulation in the drug delivery system which followed the Higuchi model with the Fickian release.

Extraction, Characterization, and Evaluation of Lepidium sativum Linn. Mucilage as a Mucoadhesive Polymer.

Being biocompatible, less toxic, cheap, easily available, and environmentally friendly, there is an increased trust in natural polymers in the drug delivery system. Mucilages, among the natural polymers, are the primary metabolites of plants that have been widely utilized in pharmaceutical manufacturing for different purposes, and mucoadhesive is one among them. The present study was designed to investigate the use of LSM as a mucoadhesive polymer using ibuprofen as a model drug. The mucilage was extracted following an aqueous extraction method and its percentage yield was found to be 13.2% w/w. Besides, three microsphere formulations of ibuprofen were prepared using synthetic polymer hydroxyl propyl methyl cellulose (HPMC) K100M and the LSM in polymer to drug ratios of 1 : 1, 1 : 5, and 3 : 5 by applying ionotropic gelation followed by solvent evaporation methods. The microspheres were evaluated for various micromeritic properties and all the formulations exhibited free-flowing properties. Optical microscopic pictures of almost all the microspheres except F3 and F6 (which had more or less spherical shapes) were found to have irregular and discrete shapes. Besides, the surfaces of all the formulations were rough in texture. The drug entrapment efficiency of the microspheres was found to be between 52.08% ± 0.80 and 87.97% ± 0.72. The in-vitrowash-off test evidenced that almost 50 percent (especially F3) of the microspheres were able to adhere up to 18 h and showed remarkable bioadhesion properties. The in-vitro drug release profile indicated that all the formulations were able to prolong their drug release up to 12 h with a non-fickian release mechanism, except for F4, which followed a fickian release. Therefore, based on the findings of this study, LSM can be used as a potential alternative mucoadhesive excipient for sustained release formulations.

Formulation and evaluation of mucoadhesive fluconazole vaginal tablets

Objective: Fluconazole is a triazole antifungal agent, and is used to treat fungal infections but because of frequent dosing and undesirable side effects it affects patient compliance. There came the need for a delivery system that can skip first pass metabolism and adhere long enough to treat the infection effectively, that was the aim for this study. Mucoadhesive drug delivery system adheres to mucous membrane and provide prolonged and sustained drug release. Method: Five formulations were formed by granulation method. The granules were then compressed and tablets were formed each of 250mg. Different evaluation parameters were determined like hardness, friability, weight variation, content uniformity, mucoadhesive strength, swelling index, dissolution and compatibility analysis. Results: The hardness (7.2-8.9kg), friability (0.02-0.05%), weight variation (0.1-0.4%), content uniformity (96.9-103%), were all in the pharmacopeial range. Dissolution was determined using rotating paddle apparatus with a phosphate buffer of 6.8 pH. Release kinetics showed that F1, F2, F3 showed Fickian release while F4 showed both Fickian and non Fickian release and F5 showed non Fickian release. Mucoadhesive strength was found to be the highest (46g) in formulation F5. The highest swelling index (70.34%) was shown by formulation F3 at 12h. Differential scanning calorimeter and Fourier transform infrared spectroscopy showed that there is no interaction between excipients. Conclusion: Hence, results showed that fluconazole vaginal tablets can be formed by using these ingredients and formulation F5 was the most optimum formulation.

Formulation and evaluation of mucoadhesive fluconazole vaginal tablets

Objective: Fluconazole is a triazole antifungal agent, and is used to treat fungal infections but because of frequent dosing and undesirable side effects it affects patient compliance. There came the need for a delivery system that can skip first pass metabolism and adhere long enough to treat the infection effectively, that was the aim for this study. Mucoadhesive drug delivery system adheres to mucous membrane and provide prolonged and sustained drug release. Method: Five formulations were formed by granulation method. The granules were then compressed and tablets were formed each of 250mg. Different evaluation parameters were determined like hardness, friability, weight variation, content uniformity, mucoadhesive strength, swelling index, dissolution and compatibility analysis. Results: The hardness (7.2-8.9kg), friability (0.02-0.05%), weight variation (0.1-0.4%), content uniformity (96.9-103%), were all in the pharmacopeial range. Dissolution was determined using rotating paddle apparatus with a phosphate buffer of 6.8 pH. Release kinetics showed that F1, F2, F3 showed Fickian release while F4 showed both Fickian and non Fickian release and F5 showed non Fickian release. Mucoadhesive strength was found to be the highest (46g) in formulation F5. The highest swelling index (70.34%) was shown by formulation F3 at 12h. Differential scanning calorimeter and Fourier transform infrared spectroscopy showed that there is no interaction between excipients. Conclusion: Hence, results showed that fluconazole vaginal tablets can be formed by using these ingredients and formulation F5 was the most optimum formulation.

Fabrication, performance and curcumin-controlled release of electrospun sarcoplasmic protein nanofiber films via layer-by-layer self-assembly

The recycling and high-value application of fish sarcoplasmic protein (FSP) from the surimi rinsing wastewater can promote the sustainable development. This work successfully fabricated monolayer nanofiber films and three-layer nanofiber films with cellulose acetate (CA) nanofibers as the outer layer to encapsulate curcumin (CUR) based on chitosan flocculated and direct freeze-dried FSP (CFSP and DFSP) through electrospinning and layer-by-layer (LBL) self-assembly, and investigated the films microstructure, performance and CUR release behavior. The nanofibers exhibited uniform, smooth, and beadless morphology, with a clear interface but strong interactions between the adjacent layers for three-layer films. The CA-CFSP/CUR-CA three-layer film possessed the best flexibility (elongation at break 6.5%), surface hydrophobicity (water contact angle 130.5° ± 2.6°) and thermal stability, suggesting its potential application in food packaging. The CUR release kinetics in all nanofiber films well fitted to First-order model, reflecting a release driven by concentration gradient. The monolayer films quickly released CUR in neutral PBS. The CA-DFSP/CUR-CA three-layer film could resist gastric acid and controllably released ∼18% CUR in the first 60 min and cumulatively up to 45.2% within 480 min, following diffusion-controlled Fickian release in simulated gastric-intestinal fluid (SGF-SIF), implying great applications potential in sustained release. This study can not only advance the surimi processing field by recovering and utilizing FSP from the surimi rinsing wastewater, but also expand the application of FSP for food packaging and drug delivery fields.

Encapsulation of Carvacrol-Loaded Nanoemulsion Obtained Using Phase Inversion Composition Method in Alginate Beads and Polysaccharide-Coated Alginate Beads.

Nanoemulsions have been widely studied as lipophilic compound loading systems. A low-energy emulsification method, phase inversion composition (PIC), was used to prepare oil-in-water nanoemulsions in a carvacrol-coconut oil/Tween 80®-(linoleic acid-potassium linoleate)/water system. The phase behaviour of several emulsification paths was studied and related to the composition range in which small-sized stable nanoemulsions could be obtained. An experimental design was carried out to determine the best formulation in terms of size and stability. Nanoemulsions with a very small mean droplet diameter (16-20 nm) were obtained and successfully encapsulated to add carvacrol to foods as a natural antimicrobial and antioxidant agent. They were encapsulated into alginate beads by external gelation. In order to improve the carvacrol kinetics release, the beads were coated with two different biopolymers: chitosan and pullulan. All formulations were analysed with scanning electron microscopy to investigate the surface morphology. The release patterns at different pHs were evaluated. Different kinetics release models were fitted in order to study the release mechanisms affecting each formulation. Chitosan-coated beads avoided the initial release burst effect, improving the beads' structure and producing a Fickian release. At basic pH, the chitosan-coated beads collapsed and the pullulan-coated beads moderately improved the release pattern of the alginate beads. For acid and neutral pHs, the chitosan-coated beads presented more sustained release patterns.

Preparation and characterization of chitosan nanoparticles loaded with Athyrium sinense essential oil with antibacterial properties against Pectobacterium carotovorum subsp. carotovorum

Pectobacterium carotovorum subsp. carotovorum (Pcc) was a pathogen that could cause serious soft rot disease of Chinese cabbage. In order to control Pcc, Athyrium sinense essential oil-loaded chitosan nanoparticles (AEO-loaded CSNPs) was obtained by embedding the Athyrium sinense essential oil (AEO) in chitosan nanoparticles (CSNPs) through ion gel method, and it was characterized and further evaluated for the antibacterial properties. The results of gas chromatography-mass spectrometer (GC-MS) analysis showed that the main components of AEO were n-hexadecanoic acid (32.18%), linoleic acid (18.28%), phytol (8.67%), fitone (4.79%), α-linolenyl alcohol (2.54%), isophytol (2.04%) and hexadecanoic acid methyl (2.03%). When chitosan (CS)/AEO ratio was 1:0.25, zeta potential was 25.7 mv, entrapment efficiency (EE) was 48.43% and loading capacity (LC) was 6.23%. These indices reached the maximum value, showing that ratio of 1:0.25 was the optimal condition for the preparation of AEO-loaded CSNPs. Therefore, AEO-loaded CSNPs prepared by using CS/AEO ratio of 1:0.25 was used for further characterization. The AEO-loaded CSNPs observed by atomic force microscopy exhibited regular shapes. Thermogravimetric analysis, fourier transform infrared, and X-ray diffraction results indicated that AEO-loaded CSNPs were effectively loaded with AEO and AEO-loaded CSNPs were successfully prepared. Finally, the antibacterial properties of AEO-loaded CSNPs were evaluated by MIC and MBC, in vitro release (within 48 h), time-kill curve (within 60 h) and in vivo experiments (within 72 h). The MIC and MBC of AEO-loaded CSNPs were 0.16 mg/mL and 0.63 mg/mL, respectively. The MIC and MBC results indicated that AEO-loaded CSNPs effectively enhanced the antibacterial activity of AEO. In vitro release results indicated that AEO-loaded CSNPs was consistent with the behavior of Fickian release and had the excellent release properties. Time-kill curve results indicated that AEO-loaded CSNPs had the characteristics of sustainability and stability. In vivo experiments (incubation for 72 h at 28 °C) showed that preventive and therapeutic effects of AEO-loaded CSNPs were 82.5% and 80.43%, which indicated that CSNP system effectively improved the in vivo effects of AEO. In conclusion, AEO-loaded CSNPs could be used as an effective antibacterial agent to control Pcc.

FORMULATION AND EVALUATION OF BILAYER TABLET OF VALSARTAN & SPIRULINA

The objective of present study was to formulate and evaluate bilayer tablet of Valsartan (VS) and Spirulina (SP) for treatment of hypertension and diabetes. The combination of Valsartan and Spirulina is used, as Valsartan establishes the immediate release layer (initial dose) and Spirulina as sustained release layer (maintenance dose) respectively. The bilayer tablets of VS and SP was particularly designed to minimize the risk of hypertension, diabetes and improve the therapeutic efficacy and to prolong the drug release and patient compliance. The formulation variables for immediate release layer include sodium starch glycolate and crospovidone as super disintegrants and micro crystalline cellulose as filer. HPMC K100, HPMC E15, was used as polymers for sustained release. The result of in-vitro release data showed that HPMC K100 can sustain the drug release up to 12hrs. From these studies HPMC K100 has been selected for further studies of bilayer tablet. Valsartan and Spirulina bilayer tablets were prepared by direct compression method. The hardness of the bilayer tablets was found to be 6.30±0.02kg/cm2. The thickness of the bilayer tablets was found to be 3.15±0.02mm. The drug content of Valsartan and Spirulina was 98.10±0.90 (SR) and 98.84±0.09 (IR). The in-vitro drug release of bilayer tablets has Valsartan immediate release was within 45minutes and Spirulina from the tablets was found sustained over 12 hours with Zero order equation to analyze the release pattern of the drug from the polymeric system. The value of “n” was in the range of 0.1531, indicating the drug release followed fickian release. Fourier transform infrared spectroscopy (FT-IR) analysis indicated that the chemical interactions between the drugs and excipients were absent. The results of Accelerated stability studies showed that all parameters were within the expected specifications and there were no significant changes observed from initial to 3 month, indicating good stability.

Nanoparticles Obtained from Zein for Encapsulation of Mesalazine.

We encapsulated MSZ in zein nanoparticles (NP-ZN) using a desolvation method followed by drying in a mini spray dryer. These nanoparticles exhibited a size of 266.6 ± 52 nm, IPD of 0.14 ± 1.1 and zeta potential of -36.4 ± 1.5 mV, suggesting colloidal stability. Quantification using HPLC showed a drug-loaded of 43.8 µg/mg. SEM demonstrated a spherical morphology with a size variation from 220 to 400 nm. A FTIR analysis did not show drug spectra in the NPs in relation to the physical mixture, which suggests drug encapsulation without changing its chemical structure. A TGA analysis showed thermal stability up to 300 °C. In vitro release studies demonstrated gastroresistance and a sustained drug release at pH 7.4 (97.67 ± 0.32%) in 120 h. The kinetic model used for the release of MSZ from the NP-ZN in a pH 1.2 medium was the Fickian diffusion, in a pH 6.8 medium it was the Peppas-Sahlin model with the polymeric relaxation mechanism and in a pH 7.4 medium it was the Korsmeyer-Peppas model with the Fickian release mechanism, or "Case I". An in vitro cytotoxicity study in the CT26.WT cell line showed no basal cytotoxicity up to 500 μg/mL. The NP-ZN showed to be a promising vector for the sustained release of MSZ in the colon by oral route.

Chitosan-based Dy2O3/CuFe3O4 bio-nanocomposite development, characterization, and drug release kinetics

Chitosan (CS)/metal oxide (MO) nano-carriers have recently attracted attention due to their great integration into several biomedical applications. Herein, CS and dysprosium oxide based bio-nanocomposites (Dy2O3/CuFe3O4/CS) were prepared using a citrate sol-gel route for biomedical settings at large and drug delivery, in particular. The chemical structure, average crystallite size, and surface morphology of Dy2O3/CuFe3O4/CS bio-nanocomposites were characterized using spectroscopic techniques, including FT-IR, PXRD, and SEM. The prepared nano composite's drug loading or release kinetics were investigated by FT-IR, zeta potential (ZP), and ultraviolet-visible spectroscopy (UV–Vis). In the FT-IR spectrum, the peaks in the range of 800–400 cm−1 confirmed the formation of meta-oxides, while amide bands at 1661 and 1638 cm−1 revealed the existence of CS in the bio-nanocomposite. The peaks at 2θ = 35.46 and 28.5, 39.4 indicated the presence and chemical interaction of Dy2O3 and CuFe3O4, respectively. The crystallite size was <20 nm. The model drug used in the loading and in vitro release assays was ciprofloxacin hydrochloride. Ciprofloxacin's CF stretch caused a modest peak to be seen at 1082 cm−1 and changed in zeta potential value from 7.90 mV to 8.88 mV endorsing that the drug had been loaded onto the nanomaterial. The loading efficiency (%) of CIP onto the composite was from 25 to 30 %, calculated from optical density measurements. Different kinetic models, such as zero-order, first-order, Higuchi, Hixon-Crowell, and Korsmeyer-Peppas, were determined to confirm the drug release mechanism. The percent (%) of drug release from the surface of Dy2O3/CuFe3O4/CS in PBS (pH 7.4), acidic (pH 2.2) and basic (pH 9.4) dissolution media were found to be 70, 28 and 20 %, respectively. Drug kinetics showed that mainly the release is fickian type followed “Fick's law of diffusion”, slightly deviated from fickian release (dissolution-dependent system). Korsmeyer-Peppas (R2 0.9773, n < 0.4) and Higuchi's (R2 0.9846) models were the best for fitting controlled drug release data. The results revealed that the Dy2O3/CuFe3O4/CS bio-nanocomposite has good potential for a controlled drug delivery system.

Enzymatic Active Release of Violacein Present in Nanostructured Lipid Carrier by Lipase Encapsulated in 3D-Bioprinted Chitosan-Hydroxypropyl Methylcellulose Matrix With Anticancer Activity.

Violacein (Viol) is a bacterial purple water-insoluble pigment synthesized by Chromobacterium violaceum and other microorganisms that display many beneficial therapeutic properties including anticancer activity. Viol was produced, purified in our laboratory, and encapsulated in a nanostructured lipid carrier (NLC). The NLC is composed of the solid lipid myristyl myristate, an oily lipid mixture composed of capric and caprylic acids, and the surfactant poloxamer P188. Dormant lipase from Rhizomucor miehei was incorporated into the NLC-Viol to develop an active release system. The NLC particle size determined by dynamic light scattering brings around 150 nm particle size and ζ≈ −9.0 mV with or without lipase, but the incorporation of lipase increase the PdI from 0.241 to 0.319 (≈32%). For scaffold development, a 2.5 hydroxypropyl methylcellulose/chitosan ratio was obtained after optimization of a composite for extrusion in a 3D-bioprinter developed and constructed in our laboratory. Final Viol encapsulation efficiency in the printings was over 90%. Kinetic release of the biodye at pH = 7.4 from the mesh containing NLC-lipase showed roughly 20% Viol fast release than without the enzyme. However, both Viol kinetic releases displayed similar profiles at pH = 5.0, where the lipase is inactive. The kinetic release of Viol from the NLC-matrices was modeled and the best correlation was found with the Korsmeyer-Peppas model (R2 = 0.95) with n < 0.5 suggesting a Fickian release of Viol from the matrices. Scanning Electron Microscope (SEM) images of the NLC-meshes showed significant differences before and after Viol’s release. Also, the presence of lipase dramatically increased the gaps in the interchain mesh. XRD and Fourier Transform Infrared (FTIR) analyses of the NLC-meshes showed a decrease in the crystalline structure of the composites with the incorporation of the NLC, and the decrease of myristyl myristate in the mesh can be attributed to the lipase activity. TGA profiles of the NLC-meshes showed high thermal stability than the individual components. Cytotoxic studies in A549 and HCT-116 cancer cell lines revealed high anticancer activity of the matrix mediated by mucoadhesive chitosan, plus the biological synergistic activities of violacein and lipase.

Boosting the Anticancer Activity of Sunitinib Malate in Breast Cancer through Lipid Polymer Hybrid Nanoparticles Approach.

In the current study, lipid-polymer hybrid nanoparticles (LPHNPs) fabricated with lipoid-90H and chitosan, sunitinib malate (SM), an anticancer drug was loaded using lecithin as a stabilizer by employing emulsion solvent evaporation technique. Four formulations (SLPN1–SLPN4) were developed by varying the concentration of chitosan polymer. Based on particle characterization, SLPN4 was optimized with size (439 ± 5.8 nm), PDI (0.269), ZP (+34 ± 5.3 mV), and EE (83.03 ± 4.9%). Further, the optimized formulation was characterized by FTIR, DSC, XRD, SEM, and in vitro release studies. In-vitro release of the drug from SPN4 was found to be 84.11 ± 2.54% as compared with pure drug SM 24.13 ± 2.67%; in 48 h, release kinetics followed the Korsmeyer–Peppas model with Fickian release mechanism. The SLPN4 exhibited a potent cytotoxicity against MCF-7 breast cancer, as evident by caspase 3, 9, and p53 activities. According to the findings, SM-loaded LPHNPs might be a promising therapy option for breast cancer.

A Water in Oil Gelled Emulsion as a Topical Release Vehicle for Curcumin

AbstractThe objective of this work is to assess the influence of the concentration of polyglycerol polyricinoleate (PGPR) (at 1%, 1.5%, and 2%) on the physical properties of water in oil gelled emulsions (W/O) and evaluates their efficiency as a delivery vehicle for curcumin. Emulsions are characterized by drop size, centrifugal test, texture, and rheology during 28 days of storage. When the surfactant concentration increases, smaller droplet sizes are obtained (&lt;5 µm), the phase separation (tested by centrifugal force) decreases from 6% to 4% with little variation of the time. The mechanical properties of emulsions show a tendency to decrease as time passed and concentration of PGPR increased. The emulsions increased viscosity as the concentration increased, but the addition of curcumin reduce the viscosity of the emulsions. About controlled release profiles, a low concentration of PGPR shows an increase in the affinity between curcumin and the emulsions, following a pseudo‐Fickian release behavior. At higher concentration of PGPR shows a decrease in the affinity between curcumin and the emulsion, displaying a Fickian release behavior. The authors were able to prepare tailor made curcumin water in oil emulsion systems for the topical release of this compound.

Design and evaluation of hyaluronic acid coated plga nanoparticles of raloxifene hydrochloride for treatment of breast cancer

Context In the present study, Hyaluronic acid coated Raloxifene loaded PLGA nanoparticles have been developed to improve the anticancer potential and reduce side effects associated with the drug. Aim and Objectives The investigation was aimed to formulate and optimize Raloxifene hydrochloride loaded PLGA nanoparticles with surface modification using hyaluronic acid as a targeting moiety. To perform physicochemical characterization, in vitro cytotoxicity study (using MCF-7), in vitro drug release study and in vivo pharmacodynamic study of optimized formulation. Methodology Raloxifene hydrochloride (RALH) loaded PLGA nanoparticles were prepared by nanoprecipitation technique, followed by surface modification with hyaluronic acid. Formulation was optimized by using 23 factorial design and characterized by physicochemical, in vitro drug release, in vitro cytotoxicity studies and in vivo pharmacokinetics. Results and discussion The particle size, PDI, zeta potential, entrapment efficiency and loading capacity of spherically shaped RALH loaded nanoparticles was 207.3 ± 4.2 d.nm, 0.218 ± 0.127, -28.3 mV, 43.75 ± 1.2% and 7.55 ± 1.14% respectively. The in-vitro drug release showed sustained release and followed Korsemeyer-Peppas model with non fickian release pattern. The in-vitro cytotoxicity study of drug loaded NPs by MTT assay on MCF-7 breast carcinoma cell showed anti-cancer activity after 48 hrs of treatment. Conclusion The results of the present investigation suggested that RALH loaded HA modified PLGA nanoparticles showed sustained drug release with anticancer activity and can be promising approach for treatment of breast cancer.

Propranolol-loaded electrospun nanofibrous wound dressing: From fabrication and characterization to preliminary wound healing evaluation.

Objective(s):The wound healing potential of beta-blocker drugs such as propranolol (PNL) has recently attracted attention. To date, incorporation of PNL into electrospun nanofibrous wound dressing mats has not been tested as a novel topical drug delivery system. Presently, electrospun nanofibrous mats loaded with PNL were fabricated, and their physicochemical properties and wound healing activities were evaluated.Materials and Methods:Polyvinyl alcohol solutions containing 0, 2% or 4% (wt/vol) PNL were electrospun into mats, and the physicochemical properties and PNL release were evaluated. In vitro biocompatibility of selected PNL-loaded mats was tested in human foreskin fibroblasts and wound healing capability was evaluated in mouse skin wounds.Results:The 4% PNL mat had thin fibers (160 nm), convincing porosity (79.5%), and good hydrophilicity (swelling: 89.1%, water contact angle: 42.1°) with little degradability (14.2%). The release of PNL was not in bursts and was best explained by the Korsmeyer–Peppas equation (R2 = 0.96, n = 0.40), suggesting Fickian release. The viability of fibroblasts was 173% on day 5 of incubation with 4% PNL mats, indicating good mat biocompatibility. In vivo treatment for 14 days with 4% PNL mats resulted in wounds with a surface area of only 9% of the original wound area. These wounds had better histopathologic characteristics and were associated with less oxidative stress.Conclusion:The wound dressing fabricated with 4% PNL showed good potential for wound healing because of a favorable drug release profile from the nanofiber scaffold, and can be considered eligible for further clinical research.

Characterization of alginate extracted from Sargassum latifolium and its use in Chlorella vulgaris growth promotion and riboflavin drug delivery

Alginates derived from macroalgae have been widely used in a variety of applications due to their stability, biodegradability and biocompatibility. Alginate was extracted from Egyptian Sargassum latifolium thallus yielding 17.5% w/w. The chemical composition of S. latifolium is rich in total sugars (41.08%) and uronic acids (47.4%); while, proteins, lipids and sulfates contents are 4.61, 1.13 and 0.09%, respectively. NMR, FTIR and TGA analyses were also performed. Crystallinity index (0.334) indicates alginate semicrystalline nature. Sodium alginate hydrolysate was evaluated as Chlorella vulgaris growth promoter. The highest stimulation (0.7 g/L biomass) was achieved by using 0.3 g/L alginate hydrolysate supplementation. The highest total soluble proteins and total carbohydrates were 179.22 mg/g dry wt and 620.33 mg/g dry wt, respectively. The highest total phenolics content (27.697 mg/g dry wt.), guaiacol peroxidase activity (2.899 µmol min−1 g−1) were recorded also to 0.3 g/L alginate hydrolysate supplementation. Riboflavin-entrapped barium alginate-Arabic gum polymeric matrix (beads) was formulated to achieve 89.15% optimum drug entrapment efficiency (EE%). All formulations exhibited prolonged riboflavin release over 120 min in simulated gastric fluid, followed Higuchi model (R2 = 0.962–0.887) and Korsmeyer–Peppas model with Fickian release (n ranges from 0.204 to 0.3885).

Electrospun Nanofibers of Polycaprolactone/Collagen as a Sustained-Release Drug Delivery System for Artemisinin.

The application of artemisinin (ART) in the treatment of malaria has been restricted to a certain degree due to its inherent limitations, such as short half-life, poor solubility, limited bioavailability, and re-crystallization. Electrospun nanofibers loaded with ART provide an excellent solution to these limitations and yield sustained drug release as well as inhibition of drug re-crystallization. In this study, ART-loaded polycaprolactone (PCL)/collagen (Col) nanofibers with different proportions of polymers were prepared. ART-loaded PCL/Col nanofibers were characterized, and further ART anti-crystallization and release behaviors were studied. SEM was used to observe the morphology of PCL/Col nanofibers. X-ray diffraction (XRD) was used to characterize the physical state of ART in ART-loaded PCL/Col nanofibers. Fourier transform infrared spectroscopy (FTIR), water contact angle measurement, weight loss, degree of swelling, and drug release experiments can verify the differences in performance of ART-loaded PCL/Col nanofibers due to different polymer ratios. The release curve was analyzed by kinetics, showing sustained release for up to 48 h, and followed the Fickian release mechanism, which was shown by the diffusion index value obtained from the Korsmeyer-Peppas equation.