scholarly journals Design of Olmesartan Medoxomil-Loaded Nanosponges for Hypertension and Lung Cancer Treatments

Polymers ◽  
2021 ◽  
Vol 13 (14) ◽  
pp. 2272
Author(s):  
Bjad K. Almutairy ◽  
Abdullah Alshetaili ◽  
Amer S. Alali ◽  
Mohammed Muqtader Ahmed ◽  
Md. Khalid Anwer ◽  
...  
Keyword(s):  
Cell Lines ◽  
Drug Loading ◽  
Entrapment Efficiency ◽  
Nitrogen Adsorption ◽  
Aqueous Solubility ◽  
Olmesartan Medoxomil ◽  
Drug Carriers ◽  
Scientific Basis ◽  
Spontaneously Hypertensive ◽  
A549 Lung

Olmesartan medoxomil (OLM) is one of the prominent antihypertensive drug that suffers from low aqueous solubility and dissolution rate leading to its low bioavailability. To improve the oral bioavailability of OLM, a delivery system based on ethylcellulose (EC, a biobased polymer) nanosponges (NSs) was developed and evaluated for cytotoxicity against the A549 lung cell lines and antihypertensive potential in a rat model. Four OLM-loaded NSs (ONS1-ONS4) were prepared and fully evaluated in terms of physicochemical properties. Among these formulations, ONS4 was regarded as the optimized formulation with particle size (487 nm), PDI (0.386), zeta potential (ζP = −18.1 mV), entrapment efficiency (EE = 91.2%) and drug loading (DL = 0.88%). In addition, a nanosized porous morphology was detected for this optimized system with NS surface area of about 63.512 m2/g, pore volume and pore radius Dv(r) of 0.149 cc/g and 15.274 Å, respectively, measured by nitrogen adsorption/desorption analysis. The observed morphology plus sustained release rate of OLM caused that the optimized formulation showed higher cytotoxicity against A549 lung cell lines in comparison to the pure OLM. Finally, this system (ONS4) reduced the systolic blood pressure (SBP) significantly (p < 0.01) as compared to control and pure OLM drug in spontaneously hypertensive rats. Overall, this study provides a scientific basis for future studies on the encapsulation efficiency of NSs as promising drug carriers for overcoming pharmacokinetic limitations.

scholarly journals Improved Dissolution of Albendazole from High Drug Loaded Ternary Solid Dispersion: Formulation and Characterization

2021 ◽  
Vol 20 (2) ◽  
pp. 149-158
Author(s):  
Shimul Halder ◽  
MAK Azad ◽  
Hrishik Iqbal ◽  
Madhabi Lata Shuma ◽  
Eva Rahman Kabir
Keyword(s):  
Solid Dispersion ◽  
Drug Loading ◽  
Aqueous Solubility ◽  
Drug Carriers ◽  
Physicochemical Characteristics ◽  
Water Soluble ◽  
Dissolution Behavior ◽  
Scanning Calorimetry ◽  
High Drug ◽  
Enhanced Solubility

Bioavailability of a poorly water-soluble drug, e.g., widely used anthelmintic drug Albendazole (ABZ), is very low and thus, to obtain an optimized therapeutic efficacy, the aqueous solubility of such drugs needs to be enhanced. The objective of this study was to develop an effective high drug-loaded solid dispersion (SD) of ABZ with two biocompatible drug carriers, namely Soluplus® and Ludiflash® to improve its physicochemical characteristics. Equilibrium solubility study was performed to choose the optimum polymer ratio among the formulations and it showed up to 50-fold enhanced solubility compared to crystalline ABZ in water. X-Ray Powder Diffraction (XRPD) and Differential Scanning Calorimetry (DSC) studies of SD-ABZ showed reduced crystallinity of ABZ in the SD. The polymeric carriers, notably Soluplus®, are thought to play a key role in the reduction of crystallinity and molecular polydispersity of ABZ. The dissolution studies in water showed improved dissolution of SD-ABZ compared to crystalline ABZ, with a quick onset of drug release followed by gradual dissolution. However, due to high drug-loading and retention of crystalline ABZ in the sample, the dissolution behavior was not as expected, and may require further studies to optimize the SD-ABZ formulation. Dhaka Univ. J. Pharm. Sci. 20(2): 149-158, 2021 (December)

scholarly journals Design and Synthesis of Lactose, Galactose and Cholic Acid Related Dual Conjugated Chitosan Derivatives as Potential Anti Liver Cancer Drug Carriers

Polymers ◽  
2021 ◽  
Vol 13 (17) ◽  
pp. 2939
Author(s):  
Yili Ding ◽  
Wutong Cui ◽  
Chamakura V. N. S. Vara Prasad ◽  
Bingyun Wang
Keyword(s):  
Liver Cancer ◽  
Cholic Acid ◽  
Entrapment Efficiency ◽  
Aqueous Solubility ◽  
Fold Increase ◽  
Drug Carriers ◽  
Cancer Drug ◽  
Chitosan Derivatives ◽  
Design And Synthesis ◽  
Electron Microscope Image

Cholic acid and galactose or lactose dual conjugated chitosan derivatives were designed and synthesized as potential anti liver cancer drug carriers, their structures were characterized through proton NMR spectra, elemental analysis, size distribution, zeta potential, and scanning electron microscope image studies. The ability of the dual conjugates to enhance the aqueous solubility of the cancer drug sorafenib was evaluated. The entrapment efficiency (EE%) and drug content (DC%) of sorafenib in the inclusion complexes were measured. The chitosan dual conjugate with cholic acid and galactose was found to be best in enhancing the aqueous solubility of sorafenib. The solubility of sorafenib in water has increased from 1.7 µg/mL to 1900 µg/mL which is equal to 1117-fold increase in its solubility due to the inclusion complex with chitosan conjugate.

scholarly journals Curcumin Nanoparticles and Their Cytotoxicity in Docetaxel-Resistant Castration-Resistant Prostate Cancer Cells

Biomedicines ◽  
2020 ◽  
Vol 8 (8) ◽  
pp. 253
Author(s):  
Irin Tanaudommongkon ◽  
Asama Tanaudommongkon ◽  
Priyanka Prathipati ◽  
Joey Trieu Nguyen ◽  
Evan T. Keller ◽  
...  
Keyword(s):  
Prostate Cancer ◽  
Cell Lines ◽  
Drug Loading ◽  
Antioxidant Properties ◽  
Entrapment Efficiency ◽  
Glycol Succinate ◽  
Castration Resistant Prostate Cancer ◽  
Castration Resistant ◽  
Cytotoxicity Studies ◽  
Pc3 Cells

Most prostate cancer patients develop resistance to anti-androgen therapy. This is referred to as castration-resistant prostate cancer (CRPC). Docetaxel (DTX) is the mainstay treatment against CRPC. However, over time patients eventually develop DTX resistance, which is the cause of the cancer-related mortality. Curcumin (CUR) as a natural compound has been shown to have very broad pharmacological activities, e.g., anti-inflammatory and antioxidant properties. However, CUR is very hydrophobic. The objective of this study was to develop CUR nanoparticles (NPs) and evaluate their cytotoxicity in DTX-resistant CRPC cells for the treatment of DTX-resistant CRPC. We tested solubility of CUR in different lipids and surfactants. Finally, Miglyol 812 and D-alpha-tocopheryl poly (ethylene glycol) succinate 1000 (TPGS) were chosen to prepare lipid-based NPs for CUR. We fully characterized CUR NPs that had particle size < 150 nm, high drug loading (7.5%), and entrapment efficiency (90%). Moreover, the CUR NPs were successfully lyophilized without using cryoprotectants. We tested the cytotoxicity of blank NPs, free CUR, and CUR NPs in sensitive DU145 and PC3 cells as well as their matching docetaxel-resistant cells. Cytotoxicity studies showed that blank NPs were very safe for all tested prostate cancer cell lines. Free CUR overcame the resistance in PC3 cells, but not in DU145 cells. In contrast, CUR NPs significantly increased CUR potency in all tested cell lines. Importantly, CUR NPs completely restored CUR potency in both resistant DU145 and PC3 cells. These results demonstrate that the CUR NPs have potential to overcome DTX resistance in CRPC.

scholarly journals Copolymeric Micelles Overcome the Oral Delivery Challenges of Amphotericin B

2020 ◽  
Vol 13 (6) ◽  
pp. 121
Author(s):  
Pataranapa Nimtrakul ◽  
Desmond B. Williams ◽  
Waree Tiyaboonchai ◽  
Clive A. Prestidge
Keyword(s):  
Amphotericin B ◽  
Oral Delivery ◽  
Polymeric Micelles ◽  
Drug Loading ◽  
Entrapment Efficiency ◽  
Aqueous Solubility ◽  
Fold Increase ◽  
Free Drug ◽  
Absorption Studies

Classified as a Biopharmaceutical Classification System (BCS) class IV drug, amphotericin B (AmB) has low aqueous solubility and low permeability leading to low oral bioavailability. To improve these limitations, this study investigated the potential of AmB-loaded polymeric micelles (AmB-PM) to increase intestinal absorption. AmB-PM were prepared with polyvinyl caprolactam–polyvinyl acetate–polyethylene glycol copolymer (Soluplus®) as a polymeric carrier and used a modified solvent diffusion and microfluidics (NanoAssemblr®) method. AmB-PM have a mean particle size of ~80 nm and are mono-disperse with a polydispersity index <0.2. The entrapment efficiency of AmB was up to 95% and achieved with a high drug loading up to ~20% (w/w) with a total amount of incorporated drug of 1.08 ± 0.01 mg/mL. Importantly, compared to free drug, AmB-PM protected AmB from degradation in an acidic (simulated gastric) environment. Viability studies in Caco-2 cells confirmed the safety/low toxicity of AmB-PM. In vitro cellular absorption studies confirmed that AmB-PM increased AmB uptake in Caco-2 cells 6-fold more than free AmB (i.e., 25% compared with 4% within 30 min). Furthermore, the permeability of AmB across Caco-2 monolayers was significantly faster (2-fold) and more pronounced for AmB-PM in comparison to free drug (3.5-fold increase). Thus, the developed AmB-PM show promise as a novel oral delivery system for AmB and justifies further investigation.

scholarly journals Polymeric Fe3O4 Conjugates with Bioactive Plant Molecules: Platforms for Antimicrobial Therapy

2021 ◽  
Vol 13 (3) ◽  
pp. 1043-1055
Author(s):  
J. Fernandes ◽  
T. Vaz ◽  
S. M. Gurav ◽  
T. S. Anvekar
Keyword(s):  
Drug Delivery ◽  
Drug Loading ◽  
Entrapment Efficiency ◽  
Drug Carriers ◽  
Bioactive Molecules ◽  
X Ray Diffraction ◽  
Antioxidant Agents ◽  
Developed Surface ◽  
Vis Spectroscopy ◽  
Drug Entrapment Efficiency

The emerging nano biosystems are competent in diagnosis, drug delivery, and monitoring of therapeutic response. Both imaging and therapeutic functions can be achieved by using nanoplatforms. These nanoplatforms promise to revolutionize the medical management of many personalized illnesses. The well-developed surface chemistry of iron oxide (Fe3O4) makes it easy to charge them with pharmaceutics, promoting them as nanoplatforms for building up nanoparticle-based drug delivery systems. The strategy to design multifunctional Fe3O4 conjugates with bioactive molecules of plant origin to show enhanced activity is reported here. The conjugation reveals the magnetic Fe3O4 core nanoparticle surface readily link to hydroxyl sites of the Dextrin molecule, which further conjugate to conjugated with Curcumin and D-Limonene, which are powerful anti-cancer, anti-inflammatory, and antioxidant agents. The structural, morphological, optical, and magnetic properties were analyzed by X-ray diffraction, FT-Infrared, HR-Tunneling Electron Microscopy, and Vibrating Sample Magnetometer techniques. The potential drug loading was measured as Drug Entrapment Efficiency using UV-Vis spectroscopy. The antibacterial property was tested on the bacterium S. aureus and E. coli. Fe3O4-Dextrin nanoconjugates proved to be efficient for loading and stabilizing Curcumin and Limonene. Thus, multifunctional Fe3O4 conjugates are explored as exciting nano-drug carriers for targeted drug delivery.

Preparation And Evaluation Of Gliptin Liposomes For Targetting Ocular Region In Neurodegeneration

2020 ◽  
Vol 10 ◽  
Author(s):  
Deepika Sharma ◽  
Swarna Raj ◽  
Manmohan Singhal ◽  
Bhavna Kumar
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Zeta Potential ◽  
Targeted Delivery ◽  
Drug Loading ◽  
Entrapment Efficiency ◽  
Drug Carriers ◽  
Fickian Diffusion ◽  
Ethanol Injection ◽  
Sustained Drug Delivery

Background: Neurodegeneration show distressing effects of miscommunications between brain cells. Insulin signaling dysregulation and small vessel disease in the base of diabetes may be important contributing factors in Alzheimer’s disease and vascular dementia. Gliptins shows role in neurodegeneration due to its neuroprotective effects. Eye is an extension of the brain. Ocular route reduces drug’s adverse effects offering advantage in minimizing risk by targeted delivery to brain. Conventional ophthalmic formulations exhibit poor bioavailability. Liposomes serves as promising active carriers of drugs to posterior segment eye disorders due to improvement in intravitreal half life and targeted sustained drug delivery to the retina. Liposomes act as drug carriers for entrapment of hydrophilic and hydrophobic drugs. Objective: The study aimed to formulate and evaluate sitagliptin liposomal formulation for sustained effect in individual suffering from neurodegeneration owing to high patient compliance especially in geriatric patient. Method: Sitagliptin liposomes were prepared by ethanol injection method and were evaluated for various physicochemical properties such as visual appearance, particle size distribution, zeta potential, % drug entrapment efficiency, % drug loading capacity and In-vitro drug release studies. Results: The optimized formulation (L-3) showed round-shaped distinct particles with good stability. The L-3 shows average diameter (281.9 nm); zeta potential (-11.9 mV); % entrapment efficiency (82.7 ± 0.89 %); % drug loading (33.11 ± 0.67 %). L-3 followed korsmeyer- peppas model with fickian diffusion transport of drug release giving n’ (0.3094), r (0.9753), with 83.78 ± 0.97 % of sustained drug release. The L-3 passes the sterility test indicating its safe use in ophthalmic purpose. Conclusion: Thus, liposomal drug delivery is highly effective approach for sustained drug delivery and minimizing the side effects of gliptins for effective therapy in neurodegeneration.

Solid Lipid Nanoparticles for Topical Delivery of Acitretin for the Treatment of Psoriasis by Design of Experiment

2020 ◽  
Vol 12 (2) ◽  
pp. 4474-4491
Author(s):  
Rajkumar Aland ◽  
Ganesan M ◽  
P. Rajeswara Rao ◽  
Bhikshapathi D. V. R. N.
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Solid Lipid Nanoparticles ◽  
Drug Loading ◽  
Entrapment Efficiency ◽  
Lipid Nanoparticles ◽  
Tem Analysis ◽  
In Vitro Drug Release ◽  
Solid Lipid

The main objective for this investigation is to develop and optimize the solid lipid nanoparticles formulation of acitretin for the effective drug delivery. Acitretin loaded SLNs were prepared by hot homogenization followed by the ultrasonication using Taguchi’s orthogonal array with eight parameters that could affect the particle size and entrapment efficiency. Based on the results from the analyses of the responses obtained from Taguchi design, three different independent variables including surfactant concentration (%), lipid to drug ratio (w/w) and sonication time (s) were selected for further investigation using central composite design. The  lipid Dynasan-116, surfactant poloxomer-188 and co surfactant egg lecithin resulted in better percent drug loading and evaluated for particle size, zeta potential, drug entrapment efficiency, in vitro drug release and stability. All parameters were found to be in an acceptable range. TEM analysis has demonstrated the presence of individual nanoparticles in spherical shape and the results were compatible with particle size measurements.  In vitro drug release of optimized SLN formulation (F2) was found to be 95.63 ± 1.52%, whereas pure drug release was 30.12 after 60 min and the major mechanism of drug release follows first order kinetics release data for optimized formulation (F2) with non-Fickian (anomalous) with a strong correlation coefficient (R2 = 0.94572) of Korsemeyer-Peppas model. The total drug content of acitretin gel formulation was found to 99.86 ± 0.012% and the diameter of gel formulation was 6.9 ± 0.021 cm and that of marketed gel was found to be 5.7 ± 0.06 cm, indicating better spreadability of SLN based gel formulation. The viscosity of gel formulation at 5 rpm was found to be 6.1 x 103 ± 0.4 x 103 cp. The release rate (flux) of acitretin across the membrane and excised skin differs significantly, which indicates about the barrier properties of skin. The flux value for SLN based gel formulation (182.754 ± 3.126 μg cm−2 h−1) was found to be higher than that for marketed gel (122.345 ± 4.786 μg cm−2 h−1). The higher flux and Kp values of SLN based gel suggest that it might be able to enter the skin easily as compared with marketed gel with an advantage of low interfacial tension of the emulsifier film that ensures an excellent contact to the skin. This topically oriented SLN based gel formulation could be useful in providing site-specific dermal treatment of psoriasis

Advances in the use of MOFs for Cancer Diagnosis and Treatment: An Overview

2020 ◽  
Vol 26 (33) ◽  
pp. 4174-4184
Author(s):  
Marina P. Abuçafy ◽  
Bruna L. da Silva ◽  
João A. Oshiro-Junior ◽  
Eloisa B. Manaia ◽  
Bruna G. Chiari-Andréo ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Delivery Systems ◽  
Rational Design ◽  
Gas Adsorption ◽  
Drug Loading ◽  
Drug Carriers ◽  
Delivery Systems ◽  
Academic Community ◽  
Anticancer Drug Delivery ◽  
Diagnostic Agents

Nanoparticles as drug delivery systems and diagnostic agents have gained much attention in recent years, especially for cancer treatment. Nanocarriers improve the therapeutic efficiency and bioavailability of antitumor drugs, besides providing preferential accumulation at the target site. Among different types of nanocarriers for drug delivery assays, metal-organic frameworks (MOFs) have attracted increasing interest in the academic community. MOFs are an emerging class of coordination polymers constructed of metal nodes or clusters and organic linkers that show the capacity to combine a porous structure with high drug loading through distinct kinds of interactions, overcoming the limitations of traditional drug carriers explored up to date. Despite the rational design and synthesis of MOFs, structural aspects and some applications of these materials like gas adsorption have already been comprehensively described in recent years; it is time to demonstrate their potential applications in biomedicine. In this context, MOFs can be used as drug delivery systems and theranostic platforms due to their ability to release drugs and accommodate imaging agents. This review describes the intrinsic characteristics of nanocarriers used in cancer therapy and highlights the latest advances in MOFs as anticancer drug delivery systems and diagnostic agents.

The Potential of Milk-derived Exosomes for Drug Delivery

2020 ◽  
Vol 17 ◽  
Author(s):  
Shuyuan Li ◽  
Yue Tang ◽  
Yushun Dou
Keyword(s):  
Drug Delivery ◽  
Oral Delivery ◽  
Therapeutic Potential ◽  
Current Knowledge ◽  
Biological Fluids ◽  
Drug Loading ◽  
Drug Carriers ◽  
Current Application ◽  
Therapeutic Benefits ◽  
Loading Methods

Background: Exosomes, one of the extracellular vesicles, are widely present in all biological fluids and play an important role in intercellular communication. Because of its hydrophobic lipid bilayer and aqueous hydrophilic core structure, it is considered a possible alternative to liposome drug delivery systems. Not only do they protect the cargo like liposomes during delivery, they are less toxic and better tolerated. However, due to the lack of sources and methods for obtaining enough exosomes, the therapeutic application of exosomes as drug carriers is limited. Methods: A literature search was performed using the ScienceDirect and PubMed electronic databases to obtain information from published literature on milk exosomes related to drug delivery. Results: Here, we briefly reviewed the current knowledge of exosomes, expounded the advantages of milk-derived exosomes over other delivery vectors, including a higher yield, the oral delivery characteristic and additional therapeutic benefits. The purification and drug loading methods of milk exosomes, and the current application of milk exosomes were also introduced. Conclusion: The emergence of milk-derived exosomes is expected to break through the limitations of exosomes as therapeutic carriers of drugs. We hope to raise awareness of the therapeutic potential of milk-derived exosomes as a new drug delivery system.

Hyaluronan based Multifunctional Nano-carriers for Combination Cancer Therapy

2020 ◽  
Vol 20 ◽  
Author(s):  
Menghan Gao ◽  
Hong Deng ◽  
Weiqi Zhang
Keyword(s):  
Cancer Therapy ◽  
Combination Therapy ◽  
Cancer Cells ◽  
Drug Loading ◽  
Tumor Therapy ◽  
Drug Carriers ◽  
Functional Sites ◽  
Therapeutic Modalities ◽  
Combination Cancer Therapy ◽  
Targeting Strategy

: Hyaluronan (HA) is a natural linear polysaccharide that has excellent hydrophilicity, biocompatibility, biodegradability, and low immunogenicity, making it one of the most attractive biopolymers used for biomedical researches and applications. Due to the multiple functional sites on HA and its intrinsic affinity for CD44, a receptor highly expressed on various cancer cells, HA has been widely engineered to construct different drug-loading nanoparticles (NPs) for CD44- targeted anti-tumor therapy. When a cocktail of drugs is co-loaded in HA NP, a multifunctional nano-carriers could be obtained, which features as a highly effective and self-targeting strategy to combat the cancers with CD44 overexpression. The HA-based multidrug nano-carriers can be a combination of different drugs, various therapeutic modalities, or the integration of therapy and diagnostics (theranostics). Up to now, there are many types of HA-based multidrug nano-carriers constructed by different formulation strategies including drug co-conjugates, micelles, nano-gels and hybrid NP of HA and so on. This multidrug nano-carrier takes the full advantages of HA as NP matrix, drug carriers and targeting ligand, representing a simplified and biocompatible platform to realize the targeted and synergistic combination therapy against the cancers. In this review, recent progresses about HA-based multidrug nano-carriers for combination cancer therapy are summarized and its potential challenges for translational applications have been discussed.

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