Higher Drug Release Rate Research Articles

Targeted Bacterial Keratitis Treatment with Polyethylene Glycol-Dithiothreitol- Boric Acid Hydrogel and Gatifloxacin.

To prolong the ocular residence time of gatifloxacin and enhance its efficacy against bacterial keratitis, this study developed a velocity-controlled polyethylene glycol-dithiothreitol- boric acid (PDB) hydrogel loaded with gatifloxacin. First, the basic properties of the synthesized PDB hydrogel and the gatifloxacin- loaded PDB hydrogel were assessed. Secondly, the in vitro degradation rate of the drugloaded PDB was measured in a simulated body fluid environment with pH 7.4/5.5. The release behavior of the drug-loaded PDB was studied using a dialysis method with PBS solution of pH 7.4/5.5 as the release medium. Finally, a mouse model of bacterial keratitis was established, and tissue morphology was observed using hematoxylin-eosin staining. Additionally, mouse tear fluid was extracted to observe the antibacterial effect of the gatifloxacin-loaded PDB hydrogel. The results showed that the PDB hydrogel had a particle size of 124.9 nm and a zeta potential of -23.3 mV, with good porosity, thermosensitivity, viscosity distribution, rheological properties, and high cell compatibility. The encapsulation of gatifloxacin did not alter the physical properties of the PDB hydrogel and maintained appropriate swelling and stability, with a high drug release rate in acidic conditions. Furthermore, animal experiments demonstrated that the gatifloxacin- loaded PDB hydrogel exhibited superior therapeutic effects compared to gatifloxacin eye drops and displayed strong antibacterial capabilities against bacterial keratitis. This study successfully synthesized PDB hydrogel and developed a gatifloxacin drug release system. The hydrogel exhibited good thermosensitivity, pH responsiveness, stability, and excellent biocompatibility, which can enhance drug retention, utilization, and therapeutic effects on the ocular surface.

Pectin/Alginate bio-nanocomposite hydrogel beads based on in-situ formed layered double hydroxide in the presence of Mentha extract: Antibacterial carrier for potential pH-responsive targeted anti-cancer drug delivery

This research presents the creation of novel pH-responsive drug delivery carriers with potential applications in cancer treatment. The study involved the Mentha Extract (ME) for the in-situ synthesis of Layered Double Hydroxide (LDH) bio nanoparticles (LDH-ME NPs). These NPs were incorporated into a biopolymeric hybrid formulation containing Pectin and Alginate to produce bio-nanocomposite hydrogel beads. The morphology and chemical composition were assessed and confirmed through various techniques. Doxorubicin (DOX) was employed as a representative anti-cancer medication to investigate the controlled drug release properties of the newly developed hydrogel beads (loading capacity: ∼92 %). In vitro experiments revealed that the drug release pattern was significantly regulated in response to pH levels (with a higher drug release rate at pH 7.4, about 89 %). The assessment for antibacterial properties validated the effective antibacterial performance of the hydrogel beads toward S. aureus and E. coli with inhibition zones about 20 mm and 14 mm, respectively. MTT assay indicated a high level of cytocompatibility with HT-29 cells (cell viability exceeding 95 %) for the blank bio-nanocomposite hydrogel beads. Conversely, bio-nanocomposite hydrogel beads loaded with DOX exhibited notable cytotoxicity (∼13 % cell viability in 15.6 µg/mL) against HT-29 cells. These findings recommend the current bio-nanocomposite as a promising bio-platform with superior antibacterial and anti-cancer properties.

Precision-engineered PEGylated liposome for dual payload delivery: enhancing efficacy of Doxorubicin hydrochloride and miR-145 mimics in breast cancer cells

Micro-145 down-regulation is frequently found in breast cancers, indicating its potential as a therapeutic target. The introduction of exogenous miR-145 directly to the tumor sites has been a hurdle due to limited delivery, low bioavailability, and hence lower therapeutic efficacy. Thus, this study aims to synthesize and characterize PEGylated liposome co-loaded with Dox-HCl and miR-145 mimics to investigate its in-vitro anti-proliferative activity against MDA-MB-231 cells. The formulations were developed using a composite central design to optimize nanoparticle size and encapsulation efficiency (EE%) of Dox-HCl and miR-145 mimics. The optimized formulation exhibited the highest desirability function (D = 0.814) and displayed excellent stability over 60 days at 4 °C, maintaining a stable nanoparticle size and zeta potential, with relative EE% of Dox-HCl and miR-145 mimics on the final incubation day 94.97 ± 0.53% and 51.96 ± 2.67%, respectively. The system displayed a higher rate of drug release within 4 h of incubation at an acidic condition. Additionally, the optimized formulation demonstrated a higher toxicity (IC50 = 0.58 μM) against MDA-MB-231 cells than the free Dox- HCl and miR-145 regimen (IC50 = 1.00 μM). Our findings suggest that PEGylated liposome is tunable for effective concurrent delivery of anticancer drugs and therapeutic miRNAs into tumor cells, necessitating further investigation.

In Vitro/In Vivo Correlation of Two Extended-Release Cilostazol Formulations.

This study aims to evaluate and determine the correlation between in vitro release and in vivo pharmacokinetics of two extended-release dosage forms of Cilostazol. In vitro release profiles for two dosage forms, tablet and capsule, were analyzed under physiologically mimicked medium conditions using the paddle and basket USP release apparatus. A single-dose, two-period crossover study design in beagle dogs was applied for the pharmacokinetic study. The fed and fast effects were considered for evaluation. Pseudo gastric release medium transfer setup study from pH 1.2 to pH 6.8 (+0.5% SLS) and pH 1.2 to pH 6.8 (+1.0% SLS) demonstrated that Pletaal® SR 200 mg capsules have higher drug release rates than Cilostan® CR 200 mg tablets. Similarly, in vivo study showed Cilostazol concentration in plasma and AUC was lower under the fast state than the fed state. The ratio of least squared geometric mean values, Cmax, AUC0-t, and AUC0-inf of Cilostazol were 2.53-fold, 2.89-fold, and 2.87-fold higher for Pletaal® SR 200 mg capsules compared with Cilostan® CR 200 mg tablets, respectively. Correlation of in vitro/in vivo data indicated that Pletal® SR 200 mg capsules have better release and pharmacodynamic effect than Cilostan® CR 200 mg tablets.

Impact of manufacturing variables on product performance of contraceptive levonorgestrel intrauterine systems

The development of Levonorgestrel Intrauterine Systems (LNG-IUSs) stands as a formidable challenge due to their intricate design and reliance on specialized manufacturing methods. Pharmaceutical manufacturers face a labyrinth of process variables that demand precise identification and comprehension to establish a robust product design to ensure consistent performance. The current manuscript navigates through this complexity, describing a small-scale processing method for LNG-IUSs via addition and condensation curing processes, as well as investigating the influence of key manufacturing variables on LNG-IUS product performance. Different mixing speeds and time exhibited distinct impact on drug content uniformity within the IUS drug-polymer reservoirs. Surprisingly, no variation in drug release rates were observed. Curing temperature and time were the critical processing parameters of IUSs which were dependent on the polymer type (polydimethylsiloxane, PDMS) and drug loading. At lower curing temperatures, crosslinking in PDMS remained relatively unaffected, irrespective of drug loading. By contrast, elevating curing temperatures resulted in a drastic reduction in PDMS crosslinking densities at higher drug loading. This was attributed to increased drug volume fraction within the matrix, impeding optimal prepolymer chain mobility and rearrangement which is crucial for complete crosslinking. Interestingly, rapid curing led to increased PDMS crystallinity, thereby retarding drug release rates while concurrently compromising mechanical properties. PDMS curing chemistry, such as condensation cure (no filler) and addition cure (cured at room temperature), did not affect drug release rates of the LNG-IUSs. In the condensation cure-based LNG-IUS, the formulations prepared without filler had higher drug release rates than those containing silica or diatomaceous earth fillers. Overall, the present study unravels the intricate interplay between PDMS characteristics, processing variables, and product performance, offering fundamental insights into product design and manufacturing of brand and generic LNG-IUS products.

Construction and evaluation of biomass-modified mesoporous silica nanoparticles as enzyme-responsive and pH-Responsive drug carriers for the controlled release of quercetin

This study constructed a biomass-modified mesoporous silica nanoparticle with enzyme-responsive and pH-responsive properties. The nanoparticles were used to evaluate the loading and release capacities of quercetin (QU). The multifunctional nanoparticles (MSN@CMCS-HA) were constructed by using hyaluronic acid (HA) and carboxymethyl chitosan (CMCS) as shells and mesoporous silica nanoparticles (MSN) as cores. The carrier's structure and properties were evaluated utilizing zeta, FTIR, TGA, XPS, XRD, BET, SEM, and TEM. The drug adsorption test revealed that the maximum equilibrium adsorption capacity of MSN@CMCS-HA for QU was 314.4 mg/g. In vitro drug release demonstrated that, under the influence of hyaluronidase (100 μg/mL) and pH of 5, the high drug release rate (63.73 %) was achieved. In addition, hemolysis and CCK8 tests confirmed the high biocompatibility of MSN@CMCS-HA. Consequently, MSN@CMCS-HA exhibited promising potential as an enzyme-responsive and pH-responsive drug carrier.

Solusomes (novel soluplus® enriched nano-vesicular carriers) for improving the oral bioavailability of Candesartan cilexetil

Candesartan cilexetil (CAN) is administered for treating hypertension and heart failure. CAN suffers poor oral bioavailability, owing to limited aqueous solubility, and first-pass metabolism. Solusomes (novel Soluplus® enriched nano-vesicular carriers) combine the merits of Soluplus®, and the traditional liposomes. They were explored to increase CAN solubility, allow a high drug release rate, and improve the oral drug bioavailability. Solusomes were developed via thin film hydration technique utilizing lipid (phosphatidylcholine; PC) and polymeric solubilizer (Soluplus®; Solu). S6 system comprising PC (0.1% w/v), CAN and Soluplus® (at 1:5 ratio; w/w), following a 5 min sonication period, was the optimum one with respect to drug entrapment efficiency (83.5 ± 2.6%), drug loading (11.9 ± 0.3%), particle size and shape (377.2 ± 12.1 nm, spherical), zeta-potential (−19.6 ± 2.1 mV), saturated drug solubility (32.09 ± 0.71 µg/mL), drug released % after 1 h (68 ± 0.9%), and stability. Significantly higher Cmax (969.12 ± 46.3 ng/mL), shorter median Tmax (1h), and improved relative bioavailability (≈ 6.8 folds) in rabbits could evidence the potential of S6 system in enhancing oral CAN bioavailability. S6 solusomes act as dual platform to improve the oral drug bioavailability and maintain effective drug concentration for a prolonged period.

Berberine loaded thermosensitive lipid nanoparticles: in vitro characterization, in silico study, and in vivo anti-arthritic effect

Thermoresponsive drug delivery systems have been used to treat diseases that cause hyperthermia or elevated body tissue temperatures, viz., rheumatoid arthritis and different cancers. The aim of the study was to enhance berberine (BER) release using thermosensitive nanostructured lipid carriers (TNLCs) through intra-articular administration for the management of arthritis. TNLCs were prepared using binary mixtures of stearic acid and decanoic acid as solid and liquid lipids, respectively. Lipid mixtures with an optimum melting point were assessed using differential scanning calorimetry studies. In vitro characterization of the BER TNLCs included particle size, zeta potential, entrapment efficiency, and drug release at 37 °C and 41 °C. Joint diameter measurement, real-time polymerase chain reaction (RT-PC) analysis, enzyme-linked immunosorbent assay (ELISA) for inflammatory markers, and histological evaluation of the dissected joints were all performed in vivo on rats with adjuvant-induced arthritis. In vitro characterization revealed negatively charged BER-loaded TNLCs with a spherical shape, particle size less than 500 nm, BER entrapment efficiency up to 79%, and a high drug release rate at an elevated temperature of 41 °C. In silico studies revealed the affinity of BER to different formula components and to the measured biomarkers. In vivo assessment of the optimum TNLCs showed that BER TNLCs were superior to the BER solution suspension regarding their effect on inflammatory biomarkers, joint diameter, and histological studies.

Ultrasound-assisted synthesis layered double hydroxide@hydroxyapatite-doxorubicin coated magnetic PEG nanocomposite: A biocompatible pH-sensitive nanocarrier for anticancer drug delivery

In this study, a biocompatible pH-sensitive system was designed based on a nano-composition of layered double hydroxide@hydroxyapatite-doxorubicin coated magnetic Fe3O4-polyethylene glycol (LDH@HAp-DOX@Fe3O4-PEG) for targeted anticancer drug delivery. The prepared nanocomposites were thoroughly characterized using various techniques. The drug encapsulation efficiency (DEE) and drug-loading content (DLC) were calculated to be ∼ 78.1 % and 7.8 % for HAp-DOX, respectively. The kinetics and in-vitro drug release studies showed that LDH@HAp-DOX@Fe3O4-PEG has a controlled release profile compared to LDH@HAp-DOX at pH 5. Alternatively, the higher drug release rate (∼68.9 %) at a low-pH environment (pH 5) than that of pH 7.4 (≤40 %) confirmed a pH-sensitive release behavior of LDH@HAp-DOX@Fe3O4-PEG. In-vitro cytotoxicity and DAPI staining analyses showed that the LDH@HAp-DOX@Fe3O4-PEG has higher toxicity (cell viability ≤ 20 % at 31.25 μg/mL) than free DOX against MCF-7 breast cancer cells. In addition, the hemolysis assay confirmed the non-hemolytic nature (≤5%) of the LDH@HAp-DOX@Fe3O4-PEG nanocarrier. Based on the obtained results, the designed nanocomposite could be proposed as a promising candidate for the targeted DOX delivery by minimizing its possible side effects.

Bioinspired fine-tuning of the mechanical rigidity of SNEDDS for the efficient crossing of multiple gastrointestinal barriers

Nanoproperties, such as size, charge, and rigidity, have been demonstrated to be crucial for nanovehicles to overcome numerous gastrointestinal obstacles. However, the facile approach of modifying the rigidity of nanovehicles remains scarce, limiting understanding of how rigidity impacts their oral delivery. Inspired by the fact that cellular phospholipid content regulates plasma membrane rigidity, the rigidity of self-nanoemulsifiying drug delivery system (SNEDDS) could be fine-tuned via phosphocholine content while their size and zeta potential remain unchanged, using insulin as a model drug. Notably, soft SNEDDS exerted longer gastrointestinal transit time, higher drug release rate, stronger gastrointestinal stability and relatively lower mucus permeation but superior epithelial transcytosis than their hard counterparts in a macropinocytosis-dependent manner. The rigidity-related enhanced transcytosis was attributed to improved endocytosis, lysosome escape capability and exocytosis. Rats with type 1 diabetes exhibited greater oral insulin absorption and blood glucose lowering effect with soft SNEDDS. This study demonstrated the regulatory role of phospholipids in nanovehicle rigidity, which could help develop mechanically optimized nanomedicines in the future.

Thymoquinone-loaded self-nano-emulsifying drug delivery system against ischemia/reperfusion injury.

In the present study, a self-nano-emulsifying drug delivery system (SNEDDS) was developed to evaluate the efficiency of thymoquinone (TQ) in hepatic ischemia/reperfusion. SNEDDS was pharmaceutically characterized to evaluate droplet size, morphology, zeta potential, thermodynamic stability, and dissolution/diffusion capacity. Animals were orally pre-treated during 10days with TQ-loaded SNEDDS. Biochemical analyses, hematoxylin-eosin staining, indirect immunofluorescence, and reverse transcription polymerase chain reaction (RT-PCR) were carried out to assess cell injury, oxidative stress, inflammation, and apoptosis. The TQ formulation showed good in vitro characteristics, including stable nanoparticle structure and size with high drug release rate. In vivo determinations revealed that TQ-loaded SNEDDS pre-treatment of rats maintained cellular integrity by decreasing transaminase (ALT and AST) release and preserving the histological characteristics of their liver. The antioxidant ability of the formulation was proven by increased SOD activity, reduced MDA concentration, and iNOS protein expression. In addition, this formulation exerted an anti-inflammatory effect evidenced by reduced plasma CRP concentration, MPO activity, and gene expressions of TLR-4, TNF-α, NF-κB, and IL-6. Finally, the TQ-loaded SNEDDS formulation promoted cell survival by enhancing the Bcl-2/Bax ratio. In conclusion, our results indicate that TQ encapsulated in SNEDDS significantly protects rat liver from I/R injury.

Optimization of O/W Emulsion Solvent Evaporation Method for Itraconazole Sustained Release Microspheres.

Itraconazole, a commonly used antifungal drug in the clinic approved by U.S. Food and Drug Administration (FDA), has been gradually found to have anti-tumor, angiogenesis inhibition and other pharmacological activities. However, its poor water solubility and potential toxicity limited its clinical application. In order to improve the water solubility and reduce the side effects caused by the high concentration of itraconazole, a novel preparation method of itraconazole sustained release microspheres was established in this study. Firstly, five kinds of polylactic acid-glycolic acid (PLGA) microspheres loaded with itraconazole were prepared by oil/water (O/W) emulsion solvent evaporation and then characterized by infrared spectroscopy. Then the particle size and morphology of the microspheres were observed by scanning electron microscope (SEM) and transmission electron microscope (TEM). After that, the particle size distribution, drug loading rate, entrapment efficiency, and drug release experiments were evaluated. Our results showed the microspheres prepared in this study had uniform particle size distribution and good integrity. Further study found that the average drug loading of the five kinds of microspheres prepared with PLGA 7505, PLGA 7510, PLGA 7520, PLGA 5020 and PLGA 0020 were 16.88, 17.72, 16.72, 16.57, and 16.64%, respectively, and the encapsulation rate all reached about 100%. More surprisingly, the release experimental results showed that the microspheres prepared with PLGA 7520 did not show sudden release, showing good sustained release performance and high drug release rate. To sum up, this study optimized the preparation method of sustained-release microspheres without sudden release, which provides a new solution for the delivery of itraconazole in the clinic.

The effect of Nano-liposomal sodium nitrite on smooth muscle cell growth in a tissue-engineered small-diameter vascular graft.

Nitric oxide is a chemical agent produced by endothelial cells in a healthy blood vessel, inhibiting the overgrowth of vascular smooth muscle cells and regulating vessel tone. Liposomes are biocompatible and biodegradable drug carriers with a similar structure to cell bilayer phospholipid membrane that can be used as useful nitric oxide carriers in vascular grafts. Using a custom-designed apparatus, the sheep carotid arteries were decellularized while still maintaining important components of the vascular extracellular matrix (ECM), allowing them to be used as small-diameter vascular grafts. A chemical signal of sodium nitrite was applied to control smooth muscle cells' behavior under static and dynamic cell culture conditions. The thin film hydration approach was used to create nano-liposomes, which were then used as sodium nitrite carriers to control the drug release rate and enhance the amount of drug loaded into the liposomes. The ratio of 80:20:2 for DPPC: Cholesterol: PEG was determined as the optimum formulation of the liposome structure with high drug encapsulation efficiency (98%) and optimum drug release rate (the drug release rate was 40%, 65%, and 83% after 24, 48, and 72h, respectively). MTT assay results showed an improvement in endothelial cell proliferation in the presence of nano-liposomal sodium nitrite (LNS) at the concentration of 0.5μg/mL. Using a suitable concentration of liposomal sodium nitrite (0.5μg/mL) put onto the constructed scaffold resulted in the controllable development of smooth muscle cells in the experiment. The culture of smooth muscle cells in a pulsatile perfusion bioreactor indicated that in the presence of synthesized liposomal sodium nitrite, the overgrowth of smooth muscle cells was inhibited in dynamic cell culture conditions. The mechanical properties of ECM graft were measured, and a multi-scale model with an accuracy of 83% was proposed to predict mechanical properties successfully. The liposomal drug-loaded small-diameter vascular graft can prevent the overgrowth of SMCs and the formation of intimal hyperplasia in the graft. Aside from that, the effect of LNS on endothelial has the potential to stimulate endothelial cell proliferation and re-endothelialization.

Formulation and Optimization of Propranolol Bilayer Tablets: A Potential Approach for Effective Management of Hypertension

The purpose of this investigation is to formulate and evaluate the antihypertensive drug propranolol hydrochloride sustained-release bilayer tablets. In this formulation, one layer provides a loading dose through the immediate release of the drug and the other layer provides a maintenance dose for up to 12 h through controlled release. Different quantities of polymers such as Kyron T-314, Hydroxypropyl methylcellulose- K4M, and ethyl cellulose were used to make bi-layer tablets by direct compression. The compatibility study of pharmaceutical excipients was conducted through Fourier transform infrared spectroscopy studies and no interaction was found. The pre-compression parameter for the angle of repose, bulk density, tapped density and compressibility index was assessed on the produced granules and the findings were good. The tablets were evaluated for the post-compression parameters for thickness, hardness, friability and in vitro release studies. In vitro dissolution study was approved out for 12 h using United States Pharmacopeia dissolution apparatus I using phosphate buffer of pH 1.2 and 6.8 as dissolution medium. Hydroxypropyl methylcellulose- K4M and ethylcellulose were used in combination in all formulations but optimized formulation propranolol hydrochloride tablet 4 showed a higher rate of drug release up to 12 h as compared to the other formulation and optimized formulations propranolol hydrochloride tablet 4 follows the Higuchi model with non-fickian diffusion based on regression coefficient of the kinetics data of cumulative drug release from the dosage form.

Advanced Solid Formulations For Vulvovaginal Candidiasis.

Vulvovaginal candidiasis (VVC) is an opportunistic and endogenous infection caused by a fungus of the Candida genus, which can cause pruritus, dysuria, vulvar edema, fissures and maceration of the vulva. The treatment of vaginal candidiasis is carried out mainly by antifungal agents of azole and polyene classes; however, fungal resistance cases have been often observed. For this reason, new therapeutic agents such as essential oils, probiotics and antimicrobial peptides are being investigated, which can be combined with conventional drugs. Local administration of antimicrobials has also been considered to allow greater control of drug delivery and reduce or avoid undesirable systemic adverse effects. Conventional dosage forms such as creams and ointments result in reduced residence time in the mucosa and non-sustained and variable drug delivery. Therefore, advanced solid formulations such as intravaginal rings, vaginal films, sponges and nanofibers have been purposed. In these systems, polymers in different ratios are combined aiming to achieve a specific drug release profile and high mucoadhesion. Overall, a more porous matrix structure leads to a higher rate of drug release and mucoadhesion. The advantages, limitations and technological aspects of each dosage form are discussed in detail in this review.

Development of nanoemulsion of antiviral drug for brain targeting in the treatment of neuro-AIDS

BackgroundDelivery of drugs via the nasal route directly to the brain utilizing the olfactory pathway is purportedly known to be a more efficient method to deliver neuro-therapeutics to the brain by circumventing the BBB, thereby increasing the bioavailability of these drugs in the brain. The main objective of the project work is to improve the bioavailability of the antiretroviral drug and to minimize the side effects of this therapy which are observed at the higher side in the chronic HIV treatment. The advantage of nasal drug delivery is its noninvasiveness and self-administration. Nanoformulation provides fast onset of action and helps to achieve site-specific delivery. In the current work, nanoemulsion formulation was developed with a ternary phase system. In vitro characterization of nanoemulsion was performed.ResultOptimized batch B2 had a zeta potential of − 18.7 mV showing a stable emulsion system and a particle size of 156.2 nmin desirable size range. Batch B2 has the least variation in globule size with PDI 0.463. Results from ex vivo studies revealed that developed nanoemulsion (B2) possessed a higher rate of drug release compared to other formulations.ConclusionPhase diagrams indicated more width of the nanoemulsion region with an increase in surfactant ratio. Stable nanoemulsion was prepared with a combination of surfactant and co-surfactants. Nanoemulsions could prove one of the best alternatives for brain delivery of potent medications.Graphical

New Water-Soluble Magnetic Field-Induced Drug Delivery System Obtained Via Preferential Molecular Marriage over Narcissistic Self-Sorting.

Nanomaterials that respond to stimuli are of considerable interest for drug delivery applications. Drug delivery has been a leading challenge when it comes to the externally triggered controlled release of hydrophobic drugs. The present paper describes a unique arrangement of polymers in a competitive environment derived from the dynamic self-sorting behavior of the hydrophobic chains of amphiphilic mPEG-PLLA and poly-l-lactic acid (PLLA)-coated iron oxide nanoparticles IONP@PLLA to achieve a core-shell structure in which the hydrophobic PLLA part acts as a dense core and poly(ethylene glycol) (PEG) as an uncrowded shell. By using irreversible covalent interactions created by hydrophobic polymer-functionalized IONPs, it was possible to selectively form socially self-sorted nanocarriers (SS-NCs) with a higher hydrophobic core than the hydrophilic shell over narcissistic self-sorted nanocarriers (NS-NCs), that is, homo-micelles of amphiphilic polymers. The higher hydrophobic core of SS-NCs is indeed helpful in achieving higher drug [doxorubicin (DOX)] loading and encapsulation efficiencies of around 17 and 90%, respectively, over 10.3 and 65.6% for NS-NCs. Furthermore, due to the presence of IONPs and the densely packed hydrophobic compartments, the controlled release of DOX was facilitated by direct magnetism and temperature stimulation when an alternating magnetic field (AMF) was applied. An appreciably higher rate of drug release (∼50%) than that without AMF (∼18%) was achieved under ambient conditions in 24 h. The present study, therefore, proposes a new drug delivery system that exceeds homo-micelles and adds an extra feature of manipulating drug release through magnetism and temperature, that is, hyperthermia.

Magneto-fluorescent superparamagnetic Fe3O4@SiO2@alginate/carbon quantum dots nanohybrid for drug delivery

Magneto-fluorescent nanohybrids are promising candidates for the application in drug delivery systems with simultaneous bioimaging. In this research, Fe3O4@SiO2 superparamagnetic nanoparticles were synthesized through the co-precipitation method to be used as a platform in drug delivery systems. The core/shell nanoparticles were coated with alginate (Fe3O4@SiO2@al). N-doped carbon quantum dots (CQDs) were also synthesized by the hydrothermal method and were used in a nanohybrid with the alginate-coated Fe3O4@SiO2 nanoparticles. The synthesized nanohybrid was used for drug loading and release experiments. Phase analysis, chemical bondings, magnetic properties, drug release characteristics, and particles’ size and morphology were studied by XRD, FTIR, VSM, UV–Vis, AFM, TEM, and FESEM techniques, respectively. TEM studies showed the successful synthesis of Fe3O4@SiO2 nanoparticles with a mean particle size of around 20 nm. The Fe3O4@SiO2@al/CQDs nanoparticles showed a saturation magnetization of 42.46 emu/g. The N-doped CQDs have fluorescence emission by excitation in the range of 210–400 nm. The synthesized nanohybrid exhibited 81% drug loading, and a 25% and 38% drug release within 48 h at a pH of 7.4 and 5.5, respectively. The higher rate of drug release in a simulated tumor environment compared to normal tissues makes multifunctional magneto-fluorescent Fe3O4@SiO2@al/CQDs nanohybrid a promising candidate for simultaneous drug delivery and bioimaging.

Nanofiber Systems as Herbal Bioactive Compounds Carriers: Current Applications in Healthcare.

Nanofibers have emerged as a potential novel platform due to their physicochemical properties for healthcare applications. Nanofibers’ advantages rely on their high specific surface-area-to-volume and highly porous mesh. Their peculiar assembly allows cell accommodation, nutrient infiltration, gas exchange, waste excretion, high drug release rate, and stable structure. This review provided comprehensive information on the design and development of natural-based polymer nanofibers with the incorporation of herbal medicines for the treatment of common diseases and their in vivo studies. Natural and synthetic polymers have been widely used for the fabrication of nanofibers capable of mimicking extracellular matrix structure. Among them, natural polymers are preferred because of their biocompatibility, biodegradability, and similarity with extracellular matrix proteins. Herbal bioactive compounds from natural extracts have raised special interest due to their prominent beneficial properties in healthcare. Nanofiber properties allow these systems to serve as bioactive compound carriers to generate functional matrices with antimicrobial, anti-inflammatory, antioxidant, antiseptic, anti-viral, and other properties which have been studied in vitro and in vivo, mostly to prove their wound healing capacity and anti-inflammation properties.

Continuous production of raloxifene hydrochloride loaded nanostructured lipid carriers using hot-melt extrusion technology

The aim of this study was to utilize a continuous process for the production of orally administered raloxifene hydrochloride (RX-HCl) loaded nanostructured lipid carrier (NLC) formulations for extended drug release using hot-melt extrusion (HME) technology coupled with probe sonication, and also to evaluate the in vitro characteristics of the prepared NLCs. Preparation of the NLCs using HME technology involved two main steps, first formation of a pre-emulsion after extrusion and then size reduction of the pre-emulsion using probe sonication to obtain the NLCs. A screw speed of 100 rpm and a barrel temperature of 85 °C, were used in the extrusion process. NLCs prepared by HME technology showed a lower particle size compared to those prepared by the conventional probe sonication method. The prepared NLCs had high entrapment efficiency values (>90%). In vitro drug release was evaluated using dialysis bag diffusion technique and USP apparatus I. Overall, the RX-HCl loaded NLCs had a higher rate of drug release than the pure drug. The release profile for the F4-3 NLC formulations and pure drug at the beginning and end of the stability study were comparable. The particle size of the prepared NLCs remained stable over the storage period and all PDI and zeta potential values were ≤ 0.5 and in the range of −15 to −30 mV, respectively, indicating good physical stability of the formulations. In summary, HME technology and probe sonication were successfully used to prepare RX-HCl loaded NLC formulations with shorter processing times as compared to the conventional probe sonication method, which makes this technique a uniquely more industry-friendly method.