Percent Drug Loading Research Articles

Development and Evaluation of Sodium Alginate/Carbopol 934P-Co-Poly (Methacrylate) Hydrogels for Localized Drug Delivery.

This research was carried out to create a pH-responsive polymeric system for the targeted drug delivery of Diloxanide furoate. It relied on sodium alginate (Na-Alg) and Carbopol 934P as building blocks. Using an aqueous free radical polymerization method, SCH1-SCH12 was created with varying polymer, MAA, and MBA input ratios. Positive outcomes were seen in the swelling and release profiles at higher pH levels. Hydrogel formation, as well as component compatibility, thermal stability, and Diloxanide furoate loading, were all validated by instrumental characterization. A drug loading percentage of 83.56% was determined, with the swelling reaching 743.19%. For the formulation with MBA, the gel fraction was 94.58%. The release of diloxanide furoate increased to 91.77% at neutral pH. The formulation containing Carbopol 934P provided the highest mucoadhesion force (3993.42 dynes/cm2). The created hydrogel has been shown to be biocompatible by toxicological testing of the network. Based on the findings, the created polymeric nexus proved promising for pH-dependent localized and regulated delivery of Diloxanide furoate.

Design and Evaluation of Solid Lipid Nanoparticles Loaded Topical Gels: Repurpose of Fluoxetine in Diabetic Wound Healing.

The current study aimed to prepare a topical gel containing solid lipid nanoparticles (SLNs) encapsulating fluoxetine for diabetic wound healing effects. Fluoxetine (FX) was loaded into SLNs by employing an emulsion solvent evaporation technique using stearic acid as a lipid, and soya lecithin as a surfactant. SLNs were then evaluated for particle size, polydispersity index (PDI), zeta potential (ZP), percent entrapment efficiency (%EE), percent drug loading (%DL), and in vitro drug release. The optimized SLN (FS3) composed of FX (100 mg), SA (150 mg), and SA (100 mg) displayed mean particle size (467.3 ± 2.2nm), PDI (0.435 ± 0.02), ZP (-32.2 ± 4.47mV), EE (95.8 ± 3.38%), and DL (16.4 ± 2.4%). FTIR and DSC studies denote drug-polymer compatibility and the amorphous nature of FX in the SLNs. The drug release at 24 h was found to be (98.89 ± 2.57%) which followed the fickian diffusion mechanism. SLN (FS3) was further loaded into carbopol gel and tested for pH, spreadability, and extrudability of pharmaceutical parameters. In-vitro release of FX from the SLN gel and plain gel was compared, diabetic wound healing gel (DWH) showed sustained drug delivery. An in vivo study was also performed for DWH gel in streptozotocin-induced diabetic rats. Histopathological examination exhibited DWH gel-treated wounds have increased hydroxyproline, cellular proliferation, a rise in the number of blood vessels, and the level of collagen synthesis. Thus, DWH gel-loaded SLN encapsulated with FX could be a potential carrier for the effective treatment and management of diabetic wounds.

Development and Optimization of Methotrexate Encapsulated Polymeric Nanocarrier by Ionic Gelation Method and its Evaluations

AbstractMethotrexate encapsulated nanocarriers (M‐CNCs) were synthesized via the ionic gelation method and using Taguchi design to optimize the formulation for; size, percent entrapment efficiency (%EE), and percent drug loading (%DL). The M‐CNCs are designed to improve therapeutic efficacy and minimize the side effect of Methotrexate. Various critical factors, such as pH, polymer to a cross‐linker ratio (v/v), and reaction time (h), are considered to investigate their influence on the selected responses during the optimization. The physicochemical properties and morphology of the optimized M‐CNCs were investigated by Dynamic light scattering, Fourier transforms infrared spectroscopy (FTIR), X‐ray diffraction, Thermogravimetric analysis, and High‐resolution transmission electron microscopy. Further, In‐vitro release, stability, pharmacokinetics, and toxicity were studied. The FTIR result revealed the cross‐linking between the drug and polymer. The nanocarrier was found to be stable with spherical morphology and crystalline nature. Optimized formulation shows, Zavg=155 nm, EE=87 %, and D=49 %. The In‐vitro drug release showed a controlled release profile of MTX up to 72 h. Pharmacokinetic evaluation of M‐CNCs in healthy Sprague Dawley rats showed an improvement in plasma drug concentration. Toxicity evaluation by the histology study revealed a healthy organ architecture and the absence of pathological lesions. Overall, the formulated M‐CNCs showed enhanced bioavailability with no toxicity.

Synthesis of Gallic Acid-Loaded Chitosan-Grafted-2-Acrylamido-2-Methylpropane Sulfonic Acid Hydrogels for Oral Controlled Drug Delivery: In Vitro Biodegradation, Antioxidant, and Antibacterial Effects.

In this study, chitosan (CS) and 2-acrylamido-2-methylpropane sulfonic acid (AMPS)-based hydrogels were formulated by the free radical polymerization technique for the controlled release of gallic acid. Fourier transform infrared spectroscopy (FTIR) confirmed the successful preparation and loading of gallic acid within the hydrogel network. Differential scanning calorimetry (DSC) and thermogravimetric analysis (TGA) confirmed the increased thermal stability of the hydrogels following the crosslinking and polymerization of chitosan and AMPS. In X-ray diffraction analysis (XRD), the crystallinity of the raw materials decreased, indicating strong crosslinking of the reagents and the formation of a new polymeric network of hydrogels. Scanning electron microscopy (SEM) revealed that the hydrogel had a rough, dense, and porous surface, which is consistent with the highly polymerized composition of the hydrogel. After 48 h, the hydrogels exhibited higher swelling at pH 1.2 (swelling ratio of 19.93%) than at pH 7.4 (swelling ratio of 15.65%). The drug release was analyzed using ultraviolet-visible (UV-Vis) spectrophotometer and demonstrated that after 48 h, gallic acid release was maximum at pH 1.2 (85.27%) compared to pH 7.4 (75.19%). The percent porosity (78.36%) and drug loading increased with the increasing concentration of chitosan and AMPS, while a decrease was observed with the increasing concentration of ethylene glycol dimethyl methacrylate (EGDMA). Crosslinking of the hydrogels increased with concentrations of chitosan and EGDMA but decreased with AMPS. In vitro studies demonstrated that the developed hydrogels were biodegradable (8.6% degradation/week) and had antimicrobial (zone of inhibition of 21 and 16 mm against Gram-positive bacteria Escherichia coli and Staphylococcus aureus as well as 13 mm against Gram-negative bacteria Pseudomonas aeruginosa, respectively) and antioxidant (73% DPPH and 70% ABTS) properties. Therefore, the prepared hydrogels could be used as an effective controlled drug delivery system.

Cationic liposomes as promising vehicles for timolol/brimonidine combination ocular delivery in glaucoma: formulation development and in vitro/in vivo evaluation.

Glaucoma is a chronic eye disease in which the pressure inside the eye increases and leads to damage to the optic nerve, and eventually causes blindness. In this disease, it is often necessary to use a multi-drug treatment system. There is a fixed combination of timolol maleate and brimonidine tartrate among the combination drugs in glaucoma treatment. Liposomes are one of the most important targeted drug delivery systems to eye tissue, which leads to improved drug permeability and durability in ocular tissue. In this study, thin layer hydration was used to make liposomal formulations containing timolol maleate (TM) and brimonidine tartrate (BT). After the necessary evaluations, one of the eight initial formulations was selected as an optimization formulation. Then, characteristics such as drug loading percentage, particle size, pH, zeta potential, and drug release were performed on the optimized formulation. The study of reducing intraocular pressure was performed on the optimized formulation. This study in total was performed on 18 rabbits in three groups. Hydroxypropyl methylcellulose (HPMC) polymer was injected into the anterior chamber to experimental induce glaucoma. The selected formulation was within the acceptable range of ocular products in terms of physical properties. HPMC polymer injection successfully induced glaucoma in the animal model, resulting in a 79% increase in intraocular pressure. The results showed that the liposomal formulation significantly reduced the intraocular pressure compared to the simple formulation of the aqueous solution, and both formulations were able to significantly reduce the intraocular pressure compared to the control group (P < 0.001). The results also showed that liposomal formulation has a therapeutic effect in reducing intraocular pressure. It seems that the selected liposomal formulation made by thin layer hydration can act as a suitable drug carrier to increase the effectiveness of the fixed combination of timolol maleate and brimonidine tartrate and be proposed as a new drug formulation for targeted and controlled drug delivery in the treatment of glaucoma.

Antimicrobial Activity of Azithromycin Encapsulated into PLGA NPs: A Potential Strategy to Overcome Efflux Resistance.

Antimicrobial resistance represents a public health problem with a major negative impact on health and socioeconomic development, and is one of the biggest threats in the modern era. This requires the discovery of new approaches to control microbial infections. Nanomedicine could be one of the promising strategies to improve the treatment of microbial infections. Polymer nanoparticles (PNPs) were reported to overcome the efflux-resistant mechanism toward chemotherapeutic agents. However, to the best of our knowledge, no studies were performed to explore their ability to overcome the efflux-resistant mechanism in bacteria. In the current study, azithromycin (AZI), a macrolide antibiotic, was encapsulated into a biocompatible polymer, poly (lactic-co-glycolic acid) (PLGA) using the nano-precipitation method. The effect of the drug to polymer ratio, surfactant, and pH of the aqueous medium on particle size and drug loading percentage (DL%) were investigated in order to maximize the DL% and control the size of NPs to be around 100 nm. The antibacterial activity of AZI-PLGA NPs was investigated against AZI-resistant bacteria; Methicillin-resistant Staphylococcus aureus (MRSA) and Enterococcus faecalis (E. faecalis), where the efflux mechanism was demonstrated to be one of the resistant mechanisms. AZI-PLGA NPs were safer than free AZI, as revealed from the cytotoxicity test, and were able to overcome the efflux-resistant mechanism, as revealed by decreasing the MIC of AZI-PLGA NPs by four times than free AZI. The MIC value reduced from 256 to 64 µg/mL and from >1000 to 256 µg/mL for MRSA and E. faecalis, respectively. Therefore, encapsulation of AZI into PNPs was shown to be a promising strategy to overcome the efflux-resistant mechanism towards AZI and improve its antibacterial effect. However, future investigations are necessary to explore the effect (if any) of particle size, surface charge, and material composition of PNPs on antibacterial activity. Moreover, it is essential to ascertain the safety profiles of these PNPs, the possibility of their large-scale manufacture, and if this concept could be extended to other antibiotics.

Development and evaluation of N-acetyl glucosamine-decorated vitamin-E-based micelles incorporating resveratrol for cancer therapy

Treatment of cancerous cells like diseases underwent huge latest advancement scenario treatments with a molecular focus targeted therapy. However, non-specifically approaches through the pharmaceutical phytochemicals help a promising alternative approach for cancers. The present research study was seeking to aim at formulating the Resveratrol (RES) loaded Vitamin-E (Vit.E) micelles to improve their bioavailability and reduce toxicity. Resveratrol is a Phyto origin anticancer constituent, lipophilic in nature, with limited water solubility, resulting in poor oral bioavailability and consequently frequent dosing. Thin-film hydration (solvent casting) technique was employed in the building of RES-loaded Vit.E micelles. Prepared micelles are characterized for various parameters and the findings of in vitro evaluation studies revealed proposed micelles having the particle size of 243.4 (d. nm), polydispersity index (PDI) 0.330, zeta potential (−12.4 mV), percentage of entrapment efficiency (80.57% ± 1.06%), and percentage of drug loading (2.77 ± 1.23%), drug release in vitro (75.96%), haemolytic activity in vitro, and cytotoxicity studies in vitro. Furthermore, DSC and P-XRD analysis demonstrated that RES was effectively encapsulated within Vit.E micelles. Drug release studies revealed that dissolution of drug was improved because of loading into micelles and Transmission electron microscopy (TEM) imaging study confirmed spherically of micelles.

Design, fabrication, optimization and characterization of memantine-loaded biodegradable PLGA nanoscaffolds for treatment of Alzheimer’s disease

This study aimed to design and develop nanoscaffolds for the controlled release of memantine by non-solvent-induced phase separation (N-TIPS) method. The development and optimization of nanoscaffolds was performed by Box–Behnken Design in which two independent formulation variables and one independent process variable: poly(lactic-co-glycolic acid) (PLGA) (X 1), Pluronics F-127 (X 2), and rotation speed (X 3) were used. The design provided 15 formulation designs which were prepared to determine the response: percentage porosity (Y 1) and drug loading (Y 2). Polynomial equations were generated and analyzed statistically to establish a relationship between independent and dependent variables and develop an optimal formulation with maximized porosity (%) and drug loading (%). The optimized formulation batch was prepared using 19.18% w/v PLGA, 4.98% w/v Pluronics at 500 rpm rotation speed and exhibited drug loading of 11.66% and porosity of 82.62%. Further, correlation between the independent and dependent variables were established and statistically analyzed by using model generated mathematical regression equations, ANOVA, residual plots, interaction plot, main effect plot, contour plot and response surface designs. The analysis of model showed the significant individual effect of PLGA and significant interactive effect of Pluronics F-127 and rotation speed on drug loading and porosity. Further, its physicochemical characterization, and in-vitro (drug release kinetics, and PAMPA study), ex-vivo (enzyme inhibition assay and pro-inflammatory cytokines study) and in-vivo (neurobehavioral and histological study) studies were performed to evaluate the potential of memantine-loaded nanoscaffolds in the treatment of Alzheimer’s disease (AD).

Development and Characterization of Floating Microspheres of Dexrabeprazole Sodium for the Treatment of Peptic Ulcer

Dexrabeprazole sodium (DEX) is R (+)-isomer of rabeprazole. DEX has been used in the treatment of gastroesophageal reflux disease by suppressing gastric acid secretion. It acts as a proton pump inhibitor of the H+ /K+ ATPase enzyme. The purpose of this research was to prepare a floating drug delivery system of DEX. The floating microspheres can be prepared for the improvement of absorption and bioavailability of DEX by retaining the system in the stomach for prolonged period of time. Floating microspheres of DEX were prepared using different polymers like ethyl cellulose, hydroxy propyl methyl cellulose by solvent diffusion-evaporation method. The drug to polymer ratio used to prepare the different formulations was 1:7. The prepared floating microspheres were characterized for shape and surface morphology, size, percent drug loading, floating behavior, percentage yield and in vitro drug release. Formulation F1 showed good results with respect to the various evaluation parameters among various batches (F1-F8). The particle size increased with increase in polymer concentration. The drug entrapment efficiency was increased with increase in concentration of polymers. Buoyancy and the in vitro drug release decreased with respect to increase in concentration of polymers. In-vitro release and release kinetics data was subjected to different dissolution models. It was concluded that developed floating microspheres of DEX offers a suitable and practical approach for prolonged release of drug over an extended period of time and thus oral bioavailability, efficacy and patient compliance is improved.&#x0D; Keywords: Dexrabeprazole sodium, Floating drug delivery system, Microspheres, Solvent diffusion-evaporation method

Efficiency of Rifampin-loaded chitosan NPs in Killing of Brucella melitensis Isolated From Aborted Sheep in Wasit Province, Iraq

Brucellosis is consider one of the utmost common bacterial infectious illness that infect man and animals. unfortunately, A worldwide community in the developing country didn't provide active assistance for reducing it spread out globally. Therefore, the aim of this study is the synthesis of chitosan nanoparticles loaded with rifampin to overcome bacterial resistance and provide high intracellular penetration and the potential for potent intracellular antibacterial activity. The study was conducted from October 2019 to September 2021, Of 57 positive clinical specimens identified in the present study, 25 (65.78%), 20 (74.07%), and 12 (66.66%) were isolated from vaginal swabs, fetal membranes, and fetal abomasum contents, respectively. From the results of SEM images of NPs, it was clear that RIF-loaded CHNPs presented irregular surfaces or rough with spherical shape and presence of some particle aggregates. The RIF-CHNPs particle size observed using SEM images was 260.54 nm, while the diameter was 150.23 nm. In addition, the antibacterial activity were also measured and the results shows that the MIC values for RIF, CHNPs and RIF-CHNPs and they were 4, 2.5 and 0.625 ug/ml, respectively. While the EE % and DL % of RIF were measured spectrophotometrically. Loaded antibiotic formulation gave good percentage of entrapment efficiency and drug loading at concentration 50 mg/ml. Then the EE % at concentration 50 mg/ml was re-estimated in different pH values and the best EE% was at pH 5. In conclusion, the antibacterial activity of drug nanocarrier against B. melitensis found that it had a relatively low MIC 0.625 ug/ml. whereas the inhibitory concentrations were about 4 μg/ml and 2.5 μg/ml for the RIF and CHTNPs, respectively. Indicating there were 6.4 times reduction in MIC for RIF-CHTNPs and 1.6 time reduction for CHTNPs comparing to MIC of antibiotic alone.

Design, Fabrication and Evaluation of Stabilized Polymeric mixed micelles for Effective Management in Cancer Therapy.

Cancer is one of the most common and fatal disease, chemotherapy is the major treatment against many cancer types. The anti-apoptotic BCL-2 protein's expression was increased in many cancer types and Venetoclax (VLX; BCL-2 inhibitor) is a small molecule, which selectively inhibits this specified protein. In order to increase the clinical performance of this promising inhibitor as a repurposed drug, polymeric mixed micelles formulations approach was explored. The Venetoclax loaded polymeric mixed micelles (VPMM) were prepared by using Pluronic® F-127 and alpha tocopherol polyethylene glycol 1000 succinate (TPGS) as excipients by thin film hydration method and characteristics. The percentage drug loading capacity, entrapment efficiency and in-vitro drug release studies were performed using HPLC method. The cytotoxicity assay, cell uptake and anticancer activities were evaluated in two different cancer cells i.e. MCF-7 (breast cancer) and A-549 (lung cancer). Particle size, polydispersity index and zeta potential of the VPMM was found to be 72.88 ± 0.09nm, 0.078 ± 0.009 and -4.29 ± 0.24mV, respectively. The entrapment efficiency and %drug loading were found to be 80.12 ± 0.23% and 2.13% ± 0.14%, respectively. The IC50 of VLX was found to be 4.78, 1.30, 0.94µg/ml at 24, 48 and 72h, respectively in MCF-7 cells and 1.24, 0.68, and 0.314µg/ml at 24, 48, and 72h, respectively in A549 cells. Whereas, IC50 of VPMM was found to be 0.42, 0.29, 0.09µg/ml at 24, 48 and 72h, respectively in MCF-7 cells and 0.85, 0.13, 0.008µg/ml at 24, 48 and 72h in A549 cells, respectively, indicating VPMM showing better anti-cancer activity compared to VLX. The VPMM showed better cytotoxicity which was further proven by other assays and explained the anti-cancer activity is shown through the generation of ROS, nuclear damage,apoptotic cell death and expression of caspase-3,7, and 9 activities in apoptotic cells. The current investigation revealed that the Venetoclax loaded polymeric mixed micelles (VPMM) revealed the enhanced therapeutic efficacy against breast and lung cancer in vitro models.

Optimization of Meloxicam Solid Dispersion Formulations for Dissolution Enhancement and Storage Stability Using 33 Full Factorial Design Based on Response Surface Methodology

This study aimed to formulate and optimize solid-dispersion of meloxicam (MX) employing response-surface-methodology (RSM). RSM allowed identification of the main effects and interactions between studied factors on MX dissolution and acceleration of the optimization process. 33 full factorial design with 27 different formulations was proposed. Effects of drug loading percentage (A), carriers’ ratio (B), method of preparation (C), and their interactions on percent MX dissolved after 10 and 30 min (Q10min & Q30min) from fresh and stored samples were studied in distilled water. The considered levels were 2.5%, 5.0%, and 7.5% (factor A), three ratios of Soluplus®/Poloxamer-407 (factor B). Physical mixture (PM), fusion method (FM), and hot-melt-extrusion (HME) were considered factor (C). Stability studies were carried out for 3 months under stress conditions. The proposed optimization design was validated by 3-extra checkpoints formulations. The optimized formulation was selected via numerical optimization and investigated by DSC, XRD, PLM, and in vitro dissolution study. Results showed that HME technique gave the highest MX dissolution rate compared to other techniques (FM & PM). At constant level of factor (C), the amount of MX dissolved increased by decreasing MX loading and increasing Soluplus in carriers’ ratio. Actual responses of the optimized formulation were in close consistency with predicted data. Amorphous form of MX in the optimized formulation was proved by DSC, XRD, and PLM. Selected factors and their levels of the optimization design were significantly valuable for demonstrating and adapting the expected formulation characteristics for rapid dissolution of MX (Q10min= 89.09%) from fresh and stored samples.Graphical abstract

Formulation Design and Evaluation of Ornidazole Microsphere in a Bioadhesive gel for Local Therapy of Vaginal Candidiasis

The aim of present work is to design a novel vaginal drug delivery system composed of Ornidazole microspheres incorporated in a bioadhesive gel. Microspheres were prepared by solvent evaporation method by using Eudragit RS 100 and Eudragit RL 100 polymers with different drug/ polymer ratios. The microspheres were found to be discrete, spherical with free flowing properties and evaluated for particle size analysis, shape (SEM), drug entrapment efficiency, percentage drug loading, and in vivo drug release studies. The selected microsphere formulation (F7 and F8, containing drug polymer ratios 1:1:1 and 1:0.25:1.75 respectively) was incorporated in a bioadhesive carbopol 934P gel. The formulation (F8.ODZ-MG) which showed maximum of 91.03% release at 8h was then subjected to stability studies and antifungal activity. The antifungal activity of the F8.ODZ-MG and placebo gel was evaluated against Candida albicans 1012 by using cup plate method. This showed that ODZ-MG was capable to control the growth of Candida albicans for more than 14h. Placebo gel did not show any zone of inhibition. Stability studies were done as per ICH guidelines for a period of 6 months. Initial and third month studies were done and evaluated for parameters such as pH, drug content, drug content uniformity, extrudability, spreadability, viscosity and in vitro drug release. The results showed that there were no significant changes in the drug content and in vitro drug release. It may be concluded from the present study that ODZ-MG can be used as a novel delivery system for local therapy of vaginal candidiasis.

Synthesis of glutamic acid/polyvinyl alcohol based hydrogels for controlled drug release: In-vitro characterization and in-vivo evaluation

The aim of the current study was to prepare glutamic acid/polyvinyl alcohol based hydrogels by the free radical polymerization technique. The FTIR analysis of glutamic acid, polyvinyl alcohol, acrylic acid, and ketorolac tromethamine indicated the development and loading of the drug by the prepared hydrogels. DSC and TGA revealed the increase in the thermal stability of glutamic acid and polyvinyl alcohol after crosslinking and polymerization process, thus revealed high thermal stability for the fabricated hydrogel as compared to hydrogel contents. XRD depicted a reduction in the crystallinity of the reagents, which indicated the strong crosslinking and formation of a new polymeric network of hydrogel. SEM indicated a hard and dense surface of the prepared hydrogel, which may be correlated with the strong polymerization among hydrogel contents. Similarly, the effects of cross-linked polymers and monomer on polymer volume fraction, dynamic swelling and in-vitro drug release studies were investigated in three different pH values i.e., pH 1.2, 4.6, and 7.4, respectively. High swelling and drug release were observed as the pH of the medium was enhanced from 1.2 to 4.6 and 7.4, thus, revealed a pH-responsive nature of the prepared hydrogels. Moreover, percent porosity and drug loading were performed for fabricated hydrogels. Increase in percent porosity and drug loading was seen with the increasing composition of glutamic acid and acrylic acid while a decrease was perceived with the increase in the composition of polyvinyl alcohol. Results of sol-gel analysis revealed an increase in the cross-linking degree of the hydrogels with the increasing composition of glutamic acid, polyvinyl alcohol, and acrylic acid, while a decrease in un-crosslinking was observed, respectively. The degradation rate of hydrogel was decreased as the compositions of glutamic acid, polyvinyl alcohol, and acrylic acid was increased, which indicated a compatible network formation of hydrogel with the incorporation of high hydrogel contents. Similarly, in-vivo study was performed on rabbits and the results of pharmacokinetic parameters indicated a controlled release of the drug from the developed hydrogels for a long period of time. HET-CAM test revealed no toxic effect of the polymeric hydrogel on the chorioallantoic membrane of the fertilized chicken eggs. Therefore, regarding the results of all studies, we can conclude that the prepared hydrogels could be used for the controlled drug delivery system.

PLGA-modified Syloid®-based microparticles for the ocular delivery of terconazole: in-vitro and in-vivo investigations

The eye is an invulnerable organ with intrinsic anatomical and physiological barriers, hindering the development of a pioneer ocular formulation. The aim of this work was to develop an efficient ocular delivery system that can augment the ocular bioavailability of the antifungal drug, terconazole. Mesoporous silica microparticles, Syloid® 244 FP were utilized as the carrier system for terconazole. Preliminary studies were carried out using different drug:Syloid® weight ratios. The optimum weight ratio was mixed with various concentrations (30 and 60%w/w) of poly (lactic-co-glycolic acid) (PLGA), ester or acid-capped and with different monomers-ratio (50:50 and 75:25) using the nano-spray dryer. Results revealed the superiority of drug:Syloid® weight ratio of 1:2 in terms of yield percentage (Y%), SPAN and drug content percentage (DC%). Furthermore, incorporation of PLGA with lower glycolic acid monomer-ratio significantly increased Y%. In contrast, increasing the glycolic acid monomer-ratio resulted in higher DC% and release efficiency percentage (RE%). Additionally, doubling PLGA concentration significantly reduced Y%, DC%, drug loading percentage (DL%) and RE%. Applying desirability function in terms of increasing DC%, DL% besides RE% and decreasing SPAN, the selected formulation was chosen for DSC, XRD and SEM investigations. Results confirmed the successful loading of amorphized terconazole on PLGA-modified Syloid® microparticles. Moreover, pharmacokinetic studies for the chosen formulation on male Albino rabbits’ eyes revealed a 2, 6.7 and 25.3-fold increase in mean residence time, Cmax and AUC0–24-values, respectively, compared to the drug suspension. PLGA-modified Syloid® microparticles represent a potential option to augment the bioavailability of ocular drugs.

Macro- and Nanoscale Effect of Ethanol on Bovine Serum Albumin Gelation and Naproxen Release.

We report extended ethanol-induced gelation procedures of bovine serum albumin (BSA) at 37 °C and investigate the release behavior of a spin-labeled naproxen derivative (SL-NPX) from these hydrogels. The macroscopic mechanical properties of these gels during formation were studied using rheology, while a nanoscopic, more molecular view was obtained by analyzing the secondary structure of the protein during gelation via infrared (ATR-IR) spectroscopy. To evaluate the potential use of BSA hydrogels in controlled drug delivery, SL-NPX-BSA interaction was investigated in detail by continuous-wave electron paramagnetic resonance (CW EPR) spectroscopy, which provides information on the interaction of the small drug molecules and the hydrogel. In addition to CW EPR spectroscopy, dynamic light scattering (DLS), which provides insight into the size and nature of released components, was applied to characterize the combined influence of incubation time, ethanol, SL-drug, and BSA concentration on release behavior. It was found that the alteration of initial drug loading percentage, hydrogel incubation time as well as BSA and alcohol concentrations affect and thus tune the release rate of SL-NPX from BSA hydrogels. These results lead to the conclusion that BSA hydrogels as controlled release systems offer a remarkable fine-tuning capability for pharmaceutical applications due to the variety of gelation parameters.

Fabrication and Characterization of Paclitaxel Loaded ATO-5 Nano-Lipid Carriers (NLC’s) for Extended Drug Release

Objective: The objective of current study was to formulate and characterize nanolipid carriers of paclitaxel with increased solubility and % release profile of the drug which leads improvement of bioavailability. Methods: It is proposed to incorporate the hydrophobic anticancer drug such as paclitaxel in NLCs to increase the bioavailability and solubility of the therapeutic agent and to assess the developed formulation’s efficacy by in-vitro drug release profile. The main intents of the study are to utilize the various attributes of the proposed biopolymer (glycerol caprate) for the preparation of NLCs to encapsulate paclitaxel. The objectives of the study are to appraise the morphological, physiochemical characteristics of the developed system with their in-vitro performance. Result: The result of the NLCs characterization was evaluated by Zeta potential, poly dispersity index (PDI), percentage entrapment efficiency, drug loading, solubility and partition co-efficient. Conclusion: The result concluded stable NLCs formulation with improved solubility and extended in-vitro drug release.

Mechanistic Approach of Nano Carriers for Targeted in Cancer Chemotherapy: A Newer Strategy for Novel Drug Delivery System.

The application of nanomedicine represents an innovative approach for the treatment in the modern field of cancer chemotherapy. In the present research work, tamoxifen citrate loaded nanolipid vesicles were prepared conjugated with phosphoethanolamine as the linker molecule, and the specific antibody was tagged with the linker molecule on the bilayer surface of the vesicles. The main objective of this study is to determine the efficacy and biological behavior of antibody conjugated nanoliposome in breast cancer cell lines. Percentage of drug loading and loading efficiency was done and their results were compared to theoretical drug loading. The average diameter of those vesicles was within the 100 nm range, which is revealed in FESEM and TEM images and their lamellarity was observed in cryo-TEM images. The hydrodynamic diameter was done by particle size analysis and the surface charge was determined by the zeta potential parameter. Predominant cellular uptake was observed for antibody conjugated nanolipid vesicles in MCF-7 and MDA-MB-453 human breast cancer cell lines. A cellular apoptosis assay was conducted by flow cytometer (FACS). All experimental data would be more beneficial for the treatment of breast cancer chemotherapy. Further studies are warranted to investigate the efficacy and safety of antibody conjugated nanolipid vesicles in vivo for breast cancer animal model.

Self-assembled dehydropeptide nanocarrier as a delivery system for antitumor drug temozolomide

Stable molecular conformation and intermolecular forces are essential for peptide self-assembly. In this study, one novel dehydropeptide (DDP) monomer (Boc-(Z)Cα,β-ΔPhe-Gly-NHMe, DDP 1) was prepared; its conformation was confirmed to be more stable than the normal peptide 2 by nuclear magnetic resonance (NMR) and X-ray crystal diffraction experiments. DDP 1 was self-assembled to one novel dehydropeptide nanomaterial (DDPN 1). Fourier transform infrared (FTIR) spectroscopy results showed that hydrogen bonding was the main driving force of self-assembly. Electron microscope images displayed that the DDPN 1 fibers were longer and more stable than peptide 2 nanomaterials. Results of cell activity and enzyme hydrolysis proved that DDPN 1 had excellent biocompatibility and resistance to the enzymatic hydrolysis of protease K. Therefore, the DDPN 1 was used to load the antitumor drug temozolomide (TMZ). Due to intermolecular hydrogen bonds formed between TMZ and DDPN 1, TMZ-loaded DDPN 1 had a high percent entrapment efficiency (EE) of 83.72 ± 4.30% (n = 8) and a percent drug loading efficiency (LE) of 6.70 ± 0.34% (n = 8), and the half-life of TMZ-loaded DDPN 1 was 2.5–3 times longer than that of TMZ at pH 7. The in vitro cell viability results revealed that TMZ-loaded DDPN 1 exhibited higher antitumor activity (IC50 = 552.1 μM) against U118-MG than that of TMZ (IC50 = 1980.1 μM), possibly because that U118-MG cells uptook more TMZ from TMZ-loaded DDPN 1 than from free TMZ directly. This study is expected to inspire the design of biocompatible nanocarriers applied for anti-enzymatic hydrolysis in drug delivery systems.

Functionalization of Multi-walled Carbon Nanotubes–Silver Nanoparticle (MWCNTs-AgNPs) as a Drug Delivery System for Ibuprofen

Nanoparticle utilization for the prevention, diagnostics, and treatment of diseases is widely known as one of the medicine branches, nanomedicine. The ability to penetrate the higher space between cells and cell walls makes nanoparticles have the potential to be used as a drug delivery system (DDS). Furthermore, various techniques can be combined with nanoparticles due to their flexibility. AgNPs are one of the interesting nanoparticles to be developed into DDS. It is because they can improve antibacterial, antiviral, antifungal, antioxidant, and physicochemical properties. In addition, AgNPs have biocompatibility that can improve drug delivery capability. On the other hand, carbon-based nanomaterials such as MWCNTs have unique properties that can be potentially used as composite materials for application as DDS. Therefore, to increase the ability of DDS, the in-situ synthesis of MWCNT-AgNPs nanocomposites was carried out. UV-Vis observed the absorption peak of the nanocomposite. The characterization of the crystal structure was performed using XRD. FESEM-EDX conducted the determination of the morphology of nanocomposite and the chemical composition. The distribution of AgNPs on the MWCNTs surface was performed by TEM. Furthermore, Raman spectroscopy was used to investigate the vibration of the MWCNT-AgNPs. Drug Loading was performed using UV-Vis measurements. The results showed that MWCNT-AgNPs as a DDS are successfully created in the drug loading stage. Drug loading stage properties are increased with the increasing loading time of Ibuprofen on MWCNT-AgNPs. The optimum percentage of drug loading for Ibuprofen by MWCNTs-AgNPs was 43.7% in a contact time of 27 hours.