Emulsion Crosslinking Technique Research Articles

RES-CMCNPs Enhance Antioxidant, Proinflammatory, and Sensitivity of Tumor Solids to γ-Irradiation in EAC-Bearing Mice.

Resveratrol (Res) is a bifunctional compound found in numerous plants, including grapes and mulberries. Nanotechnology has promising applications in medicine. The ability of various nanomaterials to serve as radiosensitizers against tumor cells were reported in several manuscripts. The present investigation aimed to assess the antitumor and radiosensitizing effects of Res-CMCNPs on EAC-bearing mice. </P> Methods: Res-CMCNPs have been developed using the CMC emulsification cross-linking technique. Entrapment efficiency (%), particle size, Polydispersity index and ZETA potential, UV, FTIR spectra, and drug release were evaluated and described for RES-CMCNPs. The radiosensitizing properties of RES-CMCNPs were also evaluated in vitro and in vivo against EAC-carrying rodents. The LD50 of Res-CMCNPs was estimated and its 1/20 LD50 was prepared for treating EAC transplanted mice. </P> Results: The results revealed that the Res-CMCNPs exhibited a high entrapment efficiency (85.46%) and a size of approximately 184.60 ±17.36 nm with zeta potential value equals -51.866 mv. Also, the UV spectra of Res and Res-CMCNPs have strong absorption at 230 and 250 nm. The percentage of resveratrol release at pHs 5.8 and 7.4 was found to be 56.73% and 51.60 %, respectively, after 24 h at 100 rpm. Also, the FTIR analysis confirmed the chemical stability of resveratrol in Res-CMCNPs cross-linking. The IC50 values of Res-CMCNPs against EAC cells viability were 32.99, 25.46, and 22.21 µg after 24-, 48- and 72 h incubation, respectively, whereas those of ResCMCNPs in combination with γ-irradiation after 6-, 10 and 12-mins exposure were 24.07, 16.06 and 7.48 µg, respectively. Also, the LD50 of Res-CMCNPs was 2180 mg/kg.b.w. The treatment of EAC-bearing mice with Res-CMCNPs plus γ-irradiation improved plasma levels of NO, caspase-3, P53 and NF-kB levels as well as liver MDA, GSH, SOD, CAT, LT-B4, aromatase, Bax, Bcl2 and TGF-β levels and exhibited more significant anticancer activity than administration of ResCMCNPs and/or exposure to γ-irradiation individually. On the other hand, administration of ResCMCNPs in combination with γ-irradiation attenuated liver mRNAs (21, 29b, 181a, and 451) gene expression. </P> Conclusion: Grafting resveratrol onto carboxymethyl chitosan appears to be a promising strategy for cancer therapy as a radiosensitizer by potentiating tumor cells' sensitivity to radiation by improving levels of proinflammatory features and antioxidant biomarkers.

Eudragit-coated chitosan-tripterygium glycoside conjugate microspheres alleviate DSS-induced experimental colitis by inhibiting the TLR4/NF-κB signaling pathway

ObjectiveTripterygium glycoside (TG) is a fat-soluble extract of Tripterygium wilfordii, with anti-inflammatory properties associated with TLR signaling pathways. This study constructed a targeted delivery system for experimental colitis, namely, eudragit (EuL)-coated chitosan (Ch)-TG conjugate microspheres (Ch-TG-MS/EuL), and evaluated its therapeutic efficacy and underlying mechanisms. MethodsCh-TG-MS was fabricated using emulsification cross-linking technique and then coated with EuL to create Ch-TG-MS/EuL. Drug release properties were assessed using a dialysis model. Additionally, the therapeutic benefits of Ch-TG-MS/EuL on colonic inflammation and its specific effect on TLR4/NF-κB signaling in intestinal mucosa were evaluated in vivo using a DSS-induced murine colitis model. ResultsThe Ch-TG-MS/EuL microspheres appeared as yellow powders with a slightly enlarged shape, rough surface, and adhesions. The Ch-TG-MS/EuL formulations also exhibited high entrapment efficiency and drug loading rate. High-performance liquid chromatography revealed that Ch-TG-MS/EuL exhibited a less intense peak than free TG, confirming that the drug is contained within the formulation. Free TG displayed explosive release within the first 5 h of administration, while Ch-TG-MS/EuL prevented the pre-mature release of TG and exhibited controllable release up to 24 h. In vivo, noticeable amelioration of intestinal mucosal tissue destruction was achieved with Ch-TG-MS/EuL compared to free TG. Additionally, immunohistochemical and western blotting results revealed that Ch-TG-MS/EuL markedly down-regulated the expression of intestinal mucosal TLR4, MyD88, and NF-κB p65. Hence, Ch-TG-MS/EuL may ameliorate the colon inflammatory response by inhibiting the hyperactivation of TLR4/NF-κB signaling. ConclusionNovel Ch-TG-MS/EuL preparation may represent a colonic delivery system for UC therapeutics by inhibiting TLR4/NF-κB hyperactivation. Data availabilityAll experimental data supporting the conclusions of this study are available from the corresponding author on reasonable request.

DACLATASVIR DIHYDROCHLORIDE MICROSPHERES, PROCESS PARAMETERS FOR ENHANCED PERMEABILITY AND LIVER TARGETING

Objectives: Daclatasavir dihydrochloride (DCLD) is used to treat hepatitis C. DCLD can be used to patients with all stages of compensated liver disease including cirrhosis. The aim of the present study was to develop DCLD microspheres to improve the permeation and maximum accumulation in the liver and in vitro evaluation. Methods: DCLD microspheres were prepared with chitosan polymer using emulsion crosslinking technique. Twelve formulations were prepared, that is, F1-F12. The microspheres were evaluated for morphology, particle size, encapsulation efficiency, % yield, and permeability. FTIR studies were conducted on optimized formulation to check the drug-excipient compatibility. Results: The particle size of microspheres was in the range of 11.50±0.08 μm to 98.50±0.05 μm. Encapsulation efficiency of the formulations was observed in the range 47.8–69.2%. The ex vivo permeation studies revealed that 83.3±0.1% of drug was diffused from microspheres in 60 min, whereas from pure drug 49±0.7% of drug was diffused in 60 min. Conclusion: DCLD microspheres were shown good permeability when compared to pure drug which will improve the absorption.

FORMULATION AND EVALUATION OF POLYMERIC MICROSPHERES USING BOX–BEHNKEN DESIGN

Objectives: The purpose of this research work was to formulate and systemically evaluate in vitro performances of polymeric microspheres of nifedipine. Methods: Nifedipine microspheres containing two polymers, poloxamer 407 and carbopol 934, were prepared by single emulsion cross-linking technique. Glutaraldehyde was selected as the cross-linking agent. A Box–Behnken design was employed to study the effect of independent variables, polymer concentration (X1), stirring speed (X2), and glutaraldehyde concentration (X3) on the dependent variables particle size, drug entrapment efficiency, and flow properties of microspheres. Results: Results of preliminary trials indicate that the polymer concentration, glutaraldehyde concentration, and stirring speed affected various characteristics of microspheres. The formulated Microspheres were discrete, spherical, and free flowing. The optimized batch exhibited with the narrow particle size of 75 μm, good flow properties, and drug entrapment efficiency of 96%. Conclusion: The polymeric microspheres of nifedipine with excellent flowability and good entrapment efficiency were successfully developed. These can be useful in improving patient compliance and bioavailability of nifedipine.

Preparation and Characterization of Curcumin and Epigallocatechin gallate co-loaded polymeric microspheres for Colonic delivery

Curcumin (CURC) is a natural polyphenolic compound obtained from Curcuma longa which shows preventive and therapeutic actions against cancer. Epigallocatechin gallate (EGCG) is a potent phytomolecule obtained from Camellia sinensis, with wide biological activity. The therapeutic effect is limited, owing to poor stability and limited membrane permeability across the intestine. The aim of this study was to develop and evaluate colon-targeted microspheres of CURC and EGCG, using natural polymers. W/O emulsion crosslinking technique was used to prepare microspheres of CURC and EGCG using interpenetrating network (IPN) of Chitosan (CS) and Gum acacia (GA) and glutaraldehyde was used as a crosslinking agent. Prepared microspheres were filled in capsules coated with Eudragit S100. The prepared microspheres were evaluated in vitro for preformulation studies, encapsulation efficiency, micromeritic properties, dissolution studies and stability studies. FTIR and DSC studies had proved that the drug and polymers are compatible. The good flow property of microspheres showed that the microspheres are not aggregated. SEM micrographs of microspheres show a rough and folded surface morphology. The microspheres are spherical and uniform in shape. Formulations showed good encapsulation efficiency. Formulation F1 to F6 showed sustained release of drug for 10 h. The in-vitro drug release of batches was best explained by Higuchi models showing anomalous diffusion mechanism. The coated batch showed better release results. The optimized formulation for a period of 3 month at 40±2°/75 ± 5% RH showed no significant changes. The current approach was helpful to develop polysaccharide based microspheres of CURC and EGCG to enhance colonic drug delivery.

Synthesis, Characterization and Investigation of Water Uptake Capacity of Gelatin Coated Gold Nanoparticles

The present research work focuses on the designing of gelatin coated-Au nanoparticles and evaluating their water imbibitions capacity at different experimental conditions. Gelatin nanoparticles were synthesized by single water in oil (W/O) emulsion cross-linking technique and gold nanoparticles by Turkvitch method. For preparing these nanocarriers, ex-situ as well as in-situ methods were adopted and the prepared gelatin coated-Au nanoparticles were characterized by FTIR, SEM, TEM, XRD and in-vitro cytotoxicity techniques. The effect of various experimental conditions, such as amount of gelatin content, pH, temperature, and simulated biological fluids were investigated on the swelling behavior of nanoparticles. The as prepared gelatin coated-Au nanoparticles could be applied as nanocarriers for delivery of anticancer drugs.

Formulation and Evaluation of Sodium Alginate and Guar Gum Based Glycyrrhizin Loaded Mucoadhesive Microspheres for Management of Peptic Ulcer

Abstract: Background: Glycyrrhizin (GZ) is a bioactive ingredient of Glycyrrhiza glabra, reported for various therapeutic effects including gastro-protection. It has been associated with low absorption, early elimination, short half-life and poor bioavailability. Objectives: Aim of the current study was to formulate GZ loaded mucoadhesive microspheres by using mucopolymers like sodium alginate and guar gum for the management of peptic ulcer. Methods: Various GZ loaded microspheres (GZ-MS1-3) were prepared by an emulsification-crosslinking technique. These formulations were developed with different proportions of guar gum and sodium alginate. The formulations were characterized and evaluated by various parameters including particle size, zeta potential, entrapment efficiency (% EE), % yield, SEM, FTIR, swelling index, mucoadhesive efficiency, in vitro drug release and in vivo antioxidant activities. Results: Result stated that suitable particle size (50.18 ± 1.15 μm), zeta potential (-31.12 ± 2.16 mV), %EE (92.67 ± 1.91) and % yield (97.45 ± 1.83) was achieved with optimized formulation, GZ-MS1. Significant (***P<0.001) swelling index (0.94 ± 0.04) and mucoadhesive efficiency (95.98 ± 3.62%) was obtained with GZ-MS1. GZ-MS1 showed maximum drug release profile (94.57 ± 4.03 %) in simulated gastric fluid (SGF, pH 1.2) at 37 ± 0.5°C for 24 h. FTIR study confirmed that there was no interaction observed between GZ and excipients. Conclusion: Sustained release profile of the optimized formulation was achieved due to significant mucoadhesive efficiency of the sodium alginate and guar gum. Thus, the mucoadhesive microspheres of GZ would be an effective strategy for the management of peptic ulcer. Key words: Mucoadhesive microspheres, Glycyrrhizin, Mucopolymers, Sodium alginate, Guar gum, Sustained release, Peptic ulcer.

Poli(Rutin) micro/nanogels for biomedical applications

Flavonoids are natural phenolic compounds that are active molecules commonly found in woody and herbaceous plants and used in natural defense mechanisms of plants against harmful microorganisms. In this research, rutin (RUT) molecule which is a natural flavonoid was bounded with epoxy groups of poly(ethylene glycol) diglycidyl ether crosslinker by using micro emulsion crosslinking technique to synthesize of poly(rutin) (p(RUT)) micro/nanogels. These p(RUT) micro/nanogels showed spherical morphologic structure with 0.3 nm-2 µm dry size range due to scanning electron microscope image. Furthermore, p(RUT) micro/nanogels was found to be in injectable size range with 548±8.9 nm average size distribution in aqueous solution depends on the dynamic light scattering (DLS) measurement. In addition, the zeta potential measurements performed at different pH conditions and potentiometric titration of the prepared p(RUT) micro/nanogels was also determined and the isoelectronic point and pKa values of these micro/nanogels was estimated as pH 2.85 and 2.16, respectively. The effects of RUT and p(RUT) micro/nanogels on α-glycosidase (AG) (EC 3.2.1.20) enzyme activity were investigated and it was found that RUT and p(RUT) micro/nanogels stimulate this enzyme. Moreover, fibrinogen interaction results showed that p(RUT) micro/nanogels were more compatible than RUT for vascular system with less interaction ability of fibrinogen of p(RUT) micro/nanogels. In addition, p(RUT) micro/nanogels observed highest antioxidant scavenging ability with 251.3±20.2 gallic acid equivalency total flavonoid content (TFC) at 250 µg/mL and reduced of 1.75±0.27 µmol Fe (III) even for 5 µg p(RUT) microgel/nanogels. Furthermore, no Fe (II) chelating activity was obtained for RUT monomer, but p(RUT) micro/nanogels showed significant Fe (II) chelating activity as 43.11±17.4 %.

The Development, Evaluation, and Antioxidant Activity Analysis of Chitosan Microcapsules Containing Red Ginger Oleoresin with Sodium Tripolyphosphate Prepared by Emulsion Cross-linking Technique

In this study, chitosan-based carrier of red ginger oleoresin was prepared using the emulsion cross-linking technique with sodium tripolyphosphate (TPP) as a cross-linking agent. The effect of chitosan and TPP concentration, as well as pH on the encapsulation efficiency, particle size and characterization of chitosan microcapsule was determined. The antioxidant activity of microcapsules was analyzed. Chitosan microcapsules containing red ginger oleoresin were produced although with non-smooth surfaces.

Pharmacokinetics and hypoglycemic effect of gliclazide loaded in Isabgol husk mucilage microparticles

Among the several therapeutic agents available for the management of diabetes mellitus, sulfonylureas such as gliclazide have several advantages. The hypoglycemic effect and bioavailability of gliclazide loaded in Isabgol husk mucilage microparticles were assessed. The hypoglycemic effect of drug-loaded microparticles was compared with that of pure gliclazide. Gliclazide was incorporated into Isabgol husk mucilage microparticles using an emulsification-crosslinking technique. Gliclazide characterization was performed using a chromatographic method. Gliclazide loading in the microparticles was up to 91.23 ± 0.981% w/w. The pharmacokinetic parameters for pure gliclazide (control) were different from those of gliclazide loaded in microparticles (test). After oral administration, the AUC0–24 h of gliclazide in blood samples of the control and test groups was 10.840 ± 0.018 and 17.608 ± 0.035 μg/(mL h), respectively. In 24 h after oral administration, the percentage reduction from the baseline glucose level in diabetic rabbits was 36.66 ± 4.509% and 98.11 ± 1.018% for the test and control groups, respectively. The prolonged hypoglycemic effect and increased bioavailability of gliclazide loaded in Isabgol husk microparticles compared with those of pure drug indicate the applicability of the microparticulate formulation as a novel anti-diabetic drug delivery system.

Development of Interpenetrating Microspheres of Chitosan and Gum Arabic for Epigallocatechin Gallate to Enhance Colonic Delivery

Epigallocatechin gallate is a potent phytomolecule with wide biological activity and is a class III drug. The therapeutic effect is limited, owing to poor stability and limited membrane permeability across the intestine. The aim of this study was to develop and evaluate colon-targeted microspheres of epigallocatechin gallate, using natural polymers. Water-in-oil emulsion crosslinking technique was used to prepare microspheres of epigallocatechin gallate using interpenetrating network of chitosan and gum acacia and glutaraldehyde was used as a crosslinking agent. Prepared microspheres were filled in capsules coated with Eudragit S100. The prepared microspheres were evaluated in vitro for preformulation studies, encapsulation efficiency, micromeritic properties, dissolution studies and stability studies. Fourier transform infrared spectroscopy and differential scanning calorimetry studies had proved that the drug and polymers are compatible. The good flow property of microspheres show that the microspheres are not aggregated. Scanning electron microscope micrographs of microspheres show a rough and folded surface morphology. The microspheres are spherical and uniform in shape. Formulations show good encapsulation efficiency. Formulation F1 to F6 show sustained release of drug for 10 h. The in vitro drug release of batch F1 to F6 were best explained by Higuchi models due to diffusion mechanism of drug release from polymeric matrix system. The selected formulation batch for a period of 3 mo at 40±2°/75±5 % RH show no significant changes. The current approach was helpful to develop polysaccharide based microspheres of epigallocatechin gallate to enhance colonic drug delivery.

In vitro investigation of swelling triggered release of 5-fluorouracil from gelatin coated gold nanoparticles

In the present study gelatin coated-gold nanoparticles were synthesized and release study of the drug “5-fluorouracil” (5-FU) was carried out in a controlled manner. Gelatin nanoparticles were prepared by single water in oil (W/O) emulsion crosslinking technique and gold (Au) nanoparticles by Turkvitch method. For preparing gelatin coated-Au nanoparticles, in situ method was adopted. The release kinetics of entrapped drug was investigated as a function of various experimental factors such as chemical composition of prepared nanoparticles, pH, temperature and simulated biological fluids as the release media. The 5-FU drug loaded nanoparticles were characterized by FTIR, SEM, TEM, XRD and in vitro cytotoxicity techniques. The drug release process was analyzed kinetically using Fickian power law, zero order, first order and Korsmeyer–Peppas models, respectively, and a correlation was established between the quantity of the released drug and swelling of the nanoparticles.

A new emulsification-crosslinking technique for preparation of physically crosslinked chitosan microspheres

A new emulsification-crosslinking method was developed for the preparation of chitosan microspheres. The new method uses an aqueous alkali–urea solution, instead of the commonly used acidic solvents, to dissolve chitosan. After emulsification, the water-in-oil droplets are solidified by heating, taking advantage of the unique in situ thermal gelling behavior of the alkaline chitosan solution, instead of by crosslinking with a usually toxic crosslinker. The size of the microspheres can be controlled by the concentration of chitosan solution, stirring speed, emulsifier concentration, and the curing temperature. The resulting microspheres are physically crosslinked, instead of chemically crosslinked, and they are ready to dissolve in dilute acetic acid. The resulting chitosan microspheres are non-toxic and can be degraded by lysozyme. Bovine serum albumin, a model protein, can be facilely loaded into the microspheres by adsorption, and then released from the microspheres.

The effect of hydrolysis of cassava starch on the characteristics of microspheres prepared by an emulsification-crosslinking method

Cassava starch was hydrolyzed with 2.2 M hydrochloric acid for different periods of time. The soluble starches obtained were subsequently used for microsphere preparation by a water-in-water emulsion crosslinking technique. The average chain lengths of starches hydrolyzed for 6, 12, 24, 36, and 48 h were 122.0, 106.3, 65.4, 33.2, and 28.3, respectively. Starches hydrolyzed for 6 and 12 h did not form regular shaped microspheres, while those hydrolyzed for 24, 36, and 48 h mostly formed separate spherical-shaped microparticles with average particle sizes of 14.6, 10.1, and 10.4 μm, respectively. The swelling power of starch microspheres (SMs) produced from 24 h hydrolyzed starch was 6.5–7.0 g/g, whereas those of SMs from 36 and 48 h hydrolyzed starch were higher and comparable (8.0–9.0 g/g). All the SMs were stable against high temperature (>140 °C). Susceptibility of the SMs to α-amylase hydrolysis decreased when the degree of starch hydrolysis increased.

Microencapsulation of Purple-Fleshed Sweet Potato Anthocyanins with Chitosan-Sodium Tripolyphosphate by Using Emulsification-Crosslinking Technique

Anthocyanins extracted from purple-fleshed sweet potato were encapsulated using emulsification-crosslinking technique with chitosan acted as polymer and sodium tripolyphosphate as cross-linker. The parameters influencing microencapsulation were investigated i.e. stirring intensity and polymer concentration, pH of polymer and crosslinker solution, and also ratio of anthocyanins extract (core) to polymer concentration by characterizing the properties of obtained microcapsules. Stirring intensity of 1600 rpm achieved microcapsules with smaller mean diameter, narrower particle size distribution, and greater encapsulation efficiency than that of 1200 rpm for each similar polymer concentration. The research revealed that pH of 3.0 gave the greatest encapsulation efficiency and antioxidant activity of microcapsules. However, the different of mean diameter and particle size distribution of microcapsules for all of pH solution variation was not significant. Ratio of anthocyanins extract to polymer concentration 75% (w/w) possessed the greatest encapsulation efficiency, the biggest mean diameter and the widest particle size distribution between all of ratio variation. Meanwhile, ratio of 150% was selected for further analysis (microstructure and FT-IR) because it gave narrower particle size distribution and smaller mean diameter with its encapsulation efficiency was only little different from others ratio. Microstructure analysis by SEM revealed sphere and irregular microparticles. FT-IR analysis revealed that that there was bonding and interaction among anthocyanin, chitosan, and tripolyphosphate ion.

Covalently polysaccharide-based alginate/chitosan hydrogel embedded alginate microspheres for BSA encapsulation and soft tissue engineering

Hydrogels based scaffolds are very promising materials for a wide range of medical applications including tissue engineering and drug delivery. This study reports a covalently cross-linked composite hydrogel embedded with microspheres basing natural polysaccharides as a protein delivery system for soft tissue engineering. This biodegradable composite hydrogel derived from water-soluble chitosan and alginate derivatives upon mixing, without addition of chemical cross-linking agents. The gelation is attributed to the Schiff-base reaction between amino and aldehyde groups of N-succinyl chitosan (N-Chi) and oxidized alginate (OAlg), respectively. Meanwhile, gel-like microspheres were prepared with a diameter of 2–10 μm by conjugating sodium alginate with Ca2+ in an aqueous emulsion via the emulsion cross-linking technique. Bull Serum Albumin (BSA) was encapsulated into alginate gel microspheres and subsequently incorporated into OAlg/N-Chi hydrogels to produce a composite scaffold. In the current work, gelation rate, morphology, mechanical properties, swelling ratio, in vitro degradation and BSA release of the composite scaffolds were examined. The results show that mechanical and stable properties of gel scaffolds can be significantly improved by embedding alginate microspheres. The alginate microspheres can serve as a filler to toughen the soft OAlg/N-Chi hydrogels. Compressive modulus of composite gel scaffolds containing 0.5 mL volume of microspheres was 57.3 KPa, which was higher than the control hydrogel without microspheres. Moreover, the controlled release of BSA encapsulated within this composite hydrogels showed significantly lower rate when compared with control hydrogel or microspheres alone. These characteristics provide a potential opportunity to use this injectable composite gel scaffold in protein delivery and soft tissue engineering applications.

Magnetically responsive release of 5-FU from superparamagnetic egg albumin coated iron oxide core-shell nanoparticles

The present study aimed at preparing egg albumin coated iron oxide (EAIO) core shell nanoparticles and evaluating their ability to release 5-FU drug under applied external magnetic field. EAIO nanoparticles were prepared by simultaneous co-precipitation and emulsion crosslinking technique and characterized by FTIR, DSC, TEM, XRD, particle size analysis and surface potential measurements. The influence of chemical composition of EAIO nanoparticles, pH and temperature of release media, presence of simulated biological fluids as the release media, and applied magnetic field was investigated on the release profiles of 5-FU drug. The drug release was analyzed kinetically using Fickan power law, zero order, first order and Korsmeyer-Peppas models and the amount of released drug was correlated and the relation was drawn between the quantity of released drug and water holding capacity of nanoparticles. The nanoparticles were judged for in vitro cytotoxicity and the chemical integrity of the drug was also accessed.

Emulsion Cross-Linking Technique for Human Fibroblast Encapsulation.

Microencapsulation with biodegradable polymers has potential application in drug and cell delivery systems and is currently used in probiotic delivery. In the present study, microcapsules of human fibroblast cells (CRL2522) were prepared by emulsion cross-linking technique. Tween 80 surfactant at a 2% concentration through phase inversion resulted in the most efficient and stable size, morphology, and the cells survival at least 50% on day 14. Emulsion cross-linking microcapsule preparation resulted in smaller and possibly more diverse particles that can be developed clinically to deliver encapsulated mammalian cells for future disease treatments.

Protective Effects on 60Co-γ Radiation Damage of Pine Cone Polyphenols from Pinus koraiensis-Loaded Chitosan Microspheres In Vivo.

A novel chitosan microsphere for encapsulating pine cone polyphenols (PP) from P. koraiensis was successfully prepared using an emulsion crosslinking technique. The characteristics of pine polyphenol-loaded microspheres (PPM) were determined using scanning electron microscopy (SEM) and a laser particle size detector. It was found that PPMs were spherical in shape with uniform particle size distribution patterns. The drug content and encapsulation rate of the microspheres were 7.47% and 73.6%, respectively, at a Ch/GA mass ratio of 0.7. The animal experiments showed that PPM had a stronger radiation protective effect than PP. PPM significantly increased the immune organ indices, the quantity of marrow DNA, the superoxide dismutase (SOD) activity, the splenocyte proliferation index, and the phagocytosis activity of monocytes. PPM also decreased the numbers of micronuclei in bone marrow cells and malondialdehyde (MDA) levels in plasma in mice exposed to 60Co γ-irradiation. In addition, gender differences in biological responses to exposure to radiation were observed.

Easy fabrication and characterization of gelatin nanocarriers and in vitro investigation of swelling controlled release dynamics of paclitaxel

The purpose of the present investigation was to prepare gelatin nanoparticles, capable of releasing the paclitaxel drug in a controllable fashion by regulating the extent of swelling of the nanoparticles. Gelatin nanoparticles were prepared by a single water in oil (W/O) emulsion crosslinking technique. The nanoparticles were characterized by FTIR, SEM, TEM, XRD, particle size analysis, and surface potential measurements. The influence of experimental conditions such as chemical composition of gelatin nanoparticles, pH, temperature, and presence of simulated biological fluids as the release media were investigated on the release profiles of paclitaxel. The drug release processes were analyzed kinetically using Ficks power law, zero-order, first-order, and Korsmeyer–Peppas models, and a correlation was drawn between the quantity of released drug and swelling of the nanoparticles. The nanoparticles were judged for in vitro cytotoxicity and the chemical stability of the drug was also accessed.