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Nanotechnology mediated drug delivery has been reported to enhance the drug efficacy, bioavailability, reduced toxicity and improve patient compliance by targeting the cells and tissues to elicit the desired pharmacological action. The main aim of the study was to formulate lovastatin loaded nanosponges and to evaluate them. Lovastatin loaded nanosponges were prepared by Emulsion solvent diffusion method using different polymers (Ethyl cellulose, Polyvinyl alcohol, β-cyclodextrin, Pluronic F68, Hydroxy Propyl β- cyclodextrin). The FTIR test is conducted as the preliminary test, by this test there was no interaction between the drug and polymers. Then nanosponges were evaluated for particle size, PDI, zeta potential, SEM, entrapment efficiency andinvitrodrug release. The particle size ranged from 295.5 to 578.8 nm, PDI ranged from 0.189 to 0.465, zeta potential from -17.3 to -35.96 mV and entrapment efficiency was ranged from 78.38 to 95.77 %. The cumulative percentage release from all nanosponges varied from 66.86 to 96.60% after 12 hours depending upon the drug and polymers ratio andF6 formulation showed highest drug release i.e., 96.60%. The release kinetic studies showed that the release first order diffusion controlled and the n value (0.6017) from the Korsmeyer-Peppa’s model indicated the release mechanism was non-fickian type.&nbsp

The present research work aimed to develop and characterize nanobubbles (NBs) for synergistic action in human cell line A549 using gefitinib and oxygen. NBs were prepared by loading oxygen in β-cyc...

The aim of this analysis is to see how effective a Nanosponge-loaded topical gel is at distributing flurbiprofen through the skin. Flurbiprofen was entrapped in Nanosponge and formulated into a gel for this purpose. Flurbiprofen Nanosponges were developed by solvent evaporation using pluronic F68 and ethyl cellulose. The particle size and entrapment quality were discovered to be in the range of 200-410 nm and 90.94% to 98.68%, respectively. For gel formulation, Nanopsonges with high entrapment efficiency and the smallest particle size (F3) were chosen based on the characterization. Using Guar gum, Carbopol, and HPMC K4M, a total of 6 formulations were produced to determine the sustained drug release and were tested for physiochemical tests, producing positive results. According to the findings of the above in vitro drug release trials, formulations containing carbopol release more drug at the end of 11 hours than other formulations and follow a zero-order with case II transport mechanism.

Recent developments in nanotechnology have made the framework for the growth of new nanoscale biomaterials with numerous potential uses in nanomedicine. The nanosponge is a new and emerging technology that can be used to target medicine delivery in a precise and regulated manner. Nanosponge is an important component of advanced medication delivery. It is a specialized assisting system for regulated medication delivery of both lipophilic and hydrophilic medicines in a regulated manner. Effective medication delivery at a specific location allowed for more exact control of release rates and boosted health-care system compliance, but the chemistry having complex shape complicated things. The invention of nanosponges, on the other hand, has provided significant approach to tackling this problem. The technology of Nanosponge has been studied widely for the delivery of drugs for oral, topical, and parental administration. Enzymes, proteins, vaccines, and antibodies can all be delivered effectively using nanosponges. It is more effective for targeted drug delivery systems because it improves solubility, bioavailability, and decreases side effects by releasing the drug at specific site. It has the ability to improve drug solubility and can be manufactured into oral, topical, and parenteral dose forms. This type of carrier system is best for drugs with low bioavailability. Nanosponges can contain both lipophilic and hydrophilic medicines. Nanosponges are extremely permeable, with a high proclivity for ensuring dynamic particles and programmable delivery. This review article discusses nanosponges in general, their advantages & disadvantages, mechanism; factors influence nanosponge, preparation methods, evaluation parameters as well as applications.

In the current study, four formulae (BNS1-BNS4) of butenafine (BTF) loaded nanosponges (NS) were fabricated by solvent emulsification technology, using different concentration of ethyl cellulose (EC) and polyvinyl alcohol (PVA) as a rate retarding polymer and surfactant, respectively. Prepared NS were characterized for particle size (PS), polydispersity index (PDI), zeta potential (ZP), entrapment efficiency (EE) and drug loading (DL). Nanocarrier BNS3 was optimized based on the particle characterizations and drug encapsulation. It was further evaluated for physicochemical characterizations; FTIR, DSC, XRD and SEM. Selected NS BNS3 composed of BTF (100 mg), EC (200 mg) and 0.3% of PVA showed, PS (543 ± 0.67 nm), PDI (0.330 ± 0.02), ZP (−33.8 ± 0.89 mV), %EE (71.3 ± 0.34%) and %DL (22.8 ± 0.67%), respectively. Fabricated NS also revealed; polymer-drug compatibility, drug-encapsulation, non-crystalline state of the drug in the spherical NS as per the physicochemical evaluations. Optimized NS (BNS3) with equivalent amount of (1%, w/w or w/v) BTF was incorporated into the (1%, w/w or w/v) carbopol gel. BTF loaded NS based gel was then evaluated for viscosity, spreadability, flux, drug diffusion, antifungal, stability and skin irritation studies. BNS3 based topical gels exhibited a flux rate of 0.18 (mg/cm2.h), drug diffusion of 89.90 ± 0.87% in 24 h with Higuchi model following anomalous non-Fickian drug release. The BNS3 based-gel could be effective against pathogenic fungal strains.

Background: Nanosponge is a novel approach to topical drug delivery, especially for fungal infections. Nanosponges are a unique class of nanoparticles with three-dimensional nanostructure and nanometers wide cavities, which can encapsulate both hydrophilic and lipophilic substances providing increased efficacy and safety. Objective: To formulate and evaluate Bifonazole loaded nanosponges in hydrogels for the treatment of fungal diseases. Methods: Bifonazole-loaded nanosponges were formulated using the emulsion solvent diffusion technique. Interaction of drug-ethyl cellulose polymer along with other excipients’ was done by using FTIR as well as DSC. The nanosponges formulations were evaluated with different parameters. Results: Particle size and Zeta potential of Bifonazole loaded nanosponges for formulations were between the range of 183.7 to 560.2 nm and –17.77 to –21.9 mV, respectively. The surface morphology of nanosponges by SEM disclosed that it was spherical and porous in nature. Drug entrapment efficiency was found to be 45.44 to 79.71%. The drug release study was done by using a phosphate buffer with a pH of 6.8. Further in vitro release data was fitted into kinetic models. The optimized formulation M6 was incorporated with hydrogels; to further evaluated using parameters such as in vitro drug release studies, viscosity, pH and skin irritation studies using rat model. Stability studies of hydrogel formulation MH2 revealed no changes in in-vitro drug release, pH and drug content study at the completion of 6 months. Conclusion: Thus, the findings indicated that the prepared Bifonazole loaded nanosponges into hydrogel were stable. Hence, it could be a suitable dosage form for the cure of fungal infections in the skin.

Cancer is the most ruinous disease globally. Natural products have impressive characteristics, such as exceptional chemical versatility, chemical and biological properties of macromolecular specificity and less toxicity which make them good leads in finding novel drugs. The phytochemicals not only help to prevent but also treat chronic cancerous conditions. The present review attempts to put forth some selected anticancer phytochemicals that had reported omics characteristic and specifically suppressed cancer with in vitro and in vivo activity. Certain issues pertaining to anticancer phytochemicals like delivery to target site in the body and achieving controlled release in order to prevent overdoses have been a major concern for medical researchers worldwide. The most conventional chemotherapy protocols for the treatment of cancer lead to adverse effects that limit biological efficacy and compromise patient outcomes. In order to defeat incompetency of current and upcoming natural anticancer agents and to attain targeted drug delivery with good efficacy and fewer side effects, there is a special focus on novel nanostructured particles and nano approaches consisting of carrier system. Recent studies have led to the discovery of mesoporous and nanoporous drug delivery mechanisms, such as inorganic or organic-based nanosponges. The metal based inorganic systems have exhibited toxicity and non-biodegradable character in vivo. As a result of problems related to inorganic systems, major shift of research from inorganic to organic nanosystems has occurred. About decades ago, researchers developed organic nanosponges to control the limitation of drug delivery and cancer therapies. This review article discusses the development and application of nanosponges encapsulated phytochemicals for cancer therapy.

Study here observes comparative effect of nanosponge loaded hydrogel of Benzydamine hydrochloride against combined effect of oro-dispersible tablet consisting of vitamin B complex; B2, B6 and B12, and Benzydamine hydrochloride loaded nanogel that was evaluated against standard to show efficacy. For this study thirty Albino Wistar male rats were selected. They were observed for healing score of the ulcers, and were analysed histologically. Rats were sacrificed on three, six, twelfth day of analysis. The histological score and the clinical examination showed that the efficacy of nanosponge hydrogel of Benzydamine hydrochloride and or odispersible tablet was effective as against the standard gel of Benzydamine hydrochloride as they release the drug in a controlled manner (due to incorporation in nanosponges) as compared to standard Benzydamine hydrochloride group. The groups treated with standard formulation, nanogel and orodispersible tablet with nanogel resulted a decrease in ulcer area after the third day and there was almost a complete healing after the twelfth day. The healing score for Benzydamine hydrochloride nanogel in combination with orodispersible tablet showed a better average healing score than the nanogel and standard. As compared to the control and blank group, standard gel, nanogel and combinative treatment showed lesser healing score. Benzydamine hydrochloride nanogel and combination treatment showed an increased state of mucosal repair, thus they can be used for treating mucosal ulcers effectively.

The major problem facing the investigators is targeted drug delivery to specific sites. The emergence of a new nanoparticles carriers known as nanosponges should address these problems. Nanosponge is a novel and arising innovation that provides for topical use controlled substance delivery. The implementation of nanosponges, its prep techniques, and assessment were addressed in this review paper. Nano-sponges play a crucial role in the controlled delivery of drugs. To guide drug delivery a wide range of drugs could be packed into nanosponge. All lipophilic and hydrophilic medicinal products could be loaded into nanosponges. The drug delivery system Nanosponge has appeared to be one of life modern science many successful sectors.

Infections caused by multidrug-resistant (MDR) bacteria present an emerging global health crisis, and the threat is intensified by the involvement of biofilms. Some biofilm infections involve more than one species; this can further challenge treatment using traditional antibiotics. Nanomaterials are being developed as alternative therapeutics to traditional antibiotics; here we report biodegradable polymer-stabilized oil-in-water nanosponges (BNS) and show their activity against dual-species bacterial biofilms. The described engineered nanosponges demonstrated broad-spectrum antimicrobial activity through prevention of dual-species biofilm formation as well as eradication of preformed biofilms. The BNS showed no toxicity against mammalian cells. Together, these data highlight the therapeutic potential of this platform.

Bortezomib (BTZ) as an anticancer drug has been used through the injection pathway.Two types of Cyclodextrin nanosponges (CDNSs) were synthesized and studied by DLS, TEM, FTIR, and DSC instruments for BTZ delivery. Both carriers were analyzed for loading efficiencies andBoth types of CDNSs, encapsulated BTZ in their nano-porous structure, but better loading was shown in CDNS 1:4. FTIR and DSC results proved considerable encapsulation of BTZ into CDNSs. The slow and prolonged release profile was observed for CDNS 1:4 in comparison with CDNS 1:2. Based onCDNS 1:4 has the ability to be introduced as a nontoxic carrier for BTZ delivery with its high loading, controlled release manner, high cellular uptake, and permeability improvement characteristics.

Objective: To design a controlled topical delivery system of lornoxicam (LX) in order to enhance skin permeation and treatment efficacy. Nanosponges were selected as a novel carrier for this purpose. Methods: Nanosponges were formulated via the emulsion solvent evaporation method using ethyl cellulose (polymer) and polyvinyl alcohol (surfactant). Nanosponge dispersions were characterized for colloidal properties, entrapment efficiency and in vitro release study. The nanosponge formulation (LS1) was then incorporated into carboxymethyl cellulose sodium hydrogels and evaluated for pH, viscosity and in vitro drug release. Skin irritation was evaluated, and anti-inflammatory activity was assessed via rat hind paw edema method. Results: Nanosponges were in the nano-sized range and attained a uniform round shape with a spongy structure. LS1exhibited the highest LX release after 6 h, so it was incorporated as hydrogel. Formulated hydrogels showed acceptable physicochemical parameters (pH, drug content and rheological properties). Skin irritation testing proved LX-loaded nanosponge hydrogel formulation (G1) to be non-irritant. In vivo study revealed an enhanced anti-inflammatory activity of G1 for 6 h (p

Non-small cell lung cancer (NSCLC) contributes to about 85% of lung cancer. By 2040, lung cancer cases estimated to rise to 3.6 million globally. Brigatinib (BG) acts as tyrosine kinase inhibitors that target the epidermal growth factor receptor of the epithelial lung cancer cells. BG loaded nanosponges (NSs) were prepared by the emulsion solvent evaporation technique using ethylcellulose (EC) and polyvinyl alcohol (PVA) as a stabilizer. Eight formulations were developed by varying the concentration of the drug (BG), EC and PVA followed by optimization through particle characterization; size, polydispersity index (PDI), zeta potential (ZP), drug entrapment and loading efficiency. The optimized formulation BGNS5 showed particles size (261.0 ± 3.5 nm), PDI (0.301) and ZP(−19.83 ± 0.06 Mv) together with entrapment efficiency (85.69 ± 0.04%) and drug loading (17.69 ± 0.01%). FTIR, DSC, XRD, and SEM showed drug-polymer compatibility, entrapment of drug in EC core, non-crystallinity of BG in NS and confirm spherical porous nature of the NS. BGNS5 reflects drug release in a sustained manner, 86.91 ± 2.12% for about 12 h. BGNS5 significantly decreased the cell viability of A549 human lung cancer cell lines with less hemolytic ratio compared to pure drug BG and EC. Based on the aforementioned results BGNS5 could be used in the effective treatment of NSCLC.

We report cellular nanosponges as an effective medical countermeasure to the SARS-CoV-2 virus. Two types of cellular nanosponges are made of the plasma membranes derived from human lung epithelial type II cells or human macrophages. These nanosponges display the same protein receptors, both identified and unidentified, required by SARS-CoV-2 for cellular entry. It is shown that, following incubation with the nanosponges, SARS-CoV-2 is neutralized and unable to infect cells. Crucially, the nanosponge platform is agnostic to viral mutations and potentially viral species, as well. As long as the target of the virus remains the identified host cell, the nanosponges will be able to neutralize the virus.

We report the development of a theranostic collagen targeted cell penetrating drug delivery system toward treatment of cardiovascular disease. Caused by the action of matrix metalloproteinases (MMP...

The rapidly growing global burden of cancer poses a major challenge to public health and demands a robust approach to access promising anticancer therapeutics. In parallel, nanotechnology approaches with various pharmacological properties offer efficacious clinical outcomes. The use of new artificial variants of nanosponges (NS) as a transporter of chemotherapeutic drugs to target cells has emerged as a very promising tool. Therefore, in this research, ethylcellulose (EC) NS were prepared using the ultrasonication assisted-emulsion solvent evaporation technique. Withaferin-A (WFA), an active ingredient in Withania somnifera, has been implanted into the nanospongic framework with enhanced anticancer properties. Inside the polymeric structure, WFA was efficiently entrapped (85 ± 11%). The drug (WFA) was found to be stable within polymeric nanosponges, as demonstrated by Fourier transform infrared (FTIR) spectroscopy and differential scanning calorimetry (DSC) studies. The WFA-NS had a diameter of 117 ± 4 nm and zeta potential of −39.02 ± 5.71 mV with a polydispersity index (PDI) of 0.419 ± 0.073. In addition, scanning electron microscopy (SEM) revealed the porous surface texture of WFA-NS. In vitro anticancer activity (SRB assay) results showed that WFA–NS exhibited almost twice the anticancer efficacy against MCF-7 cells (IC50 = 1.57 ± 0.091 µM), as quantified by flow cytometry and comet tests. Moreover, fluorescence microscopy with DAPI staining and analysis of DNA fragmentation revealed apoptosis as a mechanism of cancer cell death. The anticancer activity of WFA-NS was further determined in vivo and results were compared to cisplatin. The anticancer activity of WFA-NS was further investigated in vivo, and the data were consistent to those obtained with cisplatin. At Day 10, WFA-NS (10 mg/kg) significantly reduced tumour volume to 72 ± 6%, which was comparable to cisplatin (10 mg/kg), which reduced tumour volume to 78 ± 8%. Finally, the outcomes of molecular modeling (in silico) also suggested that WFA established a stable connection with nanosponges, generating persistent hydrophobic contacts (polar and nonpolar) and helping with the attractive delayed-release features of the formulation. Collectively, all the findings support the use of WFA in nanosponges as a prototype for cancer treatment, and opened up new avenues for increasing the efficacy of natural product-derived medications.

Type 2 diabetes mellitus has been a major health issue with increasing morbidity and mortality due to macrovascular and microvascular complications. The urgent need for improved methods to control hyperglycemic complications reiterates the development of innovative preventive and therapeutic treatment strategies. In this perspective, xanthone compounds in the pericarp of the mangosteen fruit, especially α-mangostin (MGN), have been recognized to restore damaged pancreatic β-cells for optimal insulin release. Therefore, taking advantage of the robust use of nanotechnology for targeted drug delivery, we herein report the preparation of MGN loaded nanosponges for anti-diabetic therapeutic applications. The nanosponges were prepared by quasi-emulsion solvent evaporation method. Physico-chemical characterization of formulated nanosponges with satisfactory outcomes was performed with Fourier transform infra-red (FTIR) spectroscopy, differential scanning calorimetry (DSC), and scanning electron microscopy (SEM). Zeta potential, hydrodynamic diameter, entrapment efficiency, drug release properties, and stability studies at stress conditions were also tested. Molecular docking analysis revealed significant interactions of α-glucosidase and MGN in a protein-ligand complex. The maximum inhibition by nanosponges against α-glucosidase was observed to be 0.9352 ± 0.0856 µM, 3.11-fold higher than acarbose. In vivo studies were conducted on diabetic rats and plasma glucose levels were estimated by HPLC. Collectively, our findings suggest that MGN-loaded nanosponges may be beneficial in the treatment of diabetes since they prolong the antidiabetic response in plasma and improve patient compliance by slowly releasing MGN and requiring less frequent doses, respectively.

Photodynamic therapy (PDT) has extraordinary promise for the treatment of many cancers. However, its clinical progress is impaired by the intrinsic hypoxic tumor microenvironment that limits PDT efficacy and the safety concern associated with biological specificity of photosensitizers or vehicles. Now it is demonstrated that rationally designed DNA nanosponges can load and delivery photosensitizer effectively, target tumor precisely, and relieve hypoxia-associated resistance remarkably to enhance the efficacy of PDT. Specifically, the approach exhibits a facile assembly process, provides programmable and versatile nanocarriers, and enables robust in vitro and in vivo anti-cancer efficacy with excellent biosafety. These findings represent a practical and safe approach by designer DNA nanoassemblies to combat cancer effectively and suggest a powerful strategy for broad biomedical application of PDT.

Objective: The objective of the present study was to develop and characterize an optimal stable nanosponges of Gliclazide (GLZ) by using the emulsion solvent diffusion method and aimed to increase its bioavailability and release the drug in sustained and controlled manner. Methods: The GLZ nanosponge was prepared by emulsion solvent diffusion method using different drug-polymer ratios (1:1 to 1:5) Eudragit S100 is used as a polymer. Differential scanning calorimetry (DSC) and Fourier transform infrared spectroscopy (FTIR) estimated the compatibility of GLZ with polymer. All formulations evaluated for production yield, entrapment efficiency, in vitro drug release, scanning electron microscopy (SEM) and stability studies. Results: The DSC and FTIR Studies revealed that no interaction between drug and polymer. The Production yield of all batches in the range of 73.8±0.30 to 85.6±0.32. Batch F3 showed the highest production yield, the entrapment efficiency of batch F3 70.6±0.77. The average particle size ranges from 303±2.36 to 680±2.50 nm. By the end of 10th hour F3 formulation shown highest drug release was found to be 94.40±1.12%. The release kinetics of the optimized formulation shows zero-order drug release. The stability study indicates no significant change in the in vitro dissolution profile of optimized formulation. Conclusion: The results of various evaluation parameters, revealed that GLZ nanosponges would be possible alternative delivery systems to conventional formulation to improve its bioavailability, the emulsion solvent diffusion method is best method for preparation of nanosponges and release the drug in sustained and controlled manner.

Four mixed cyclodextrin-calixarene nanosponges were tested as possible Drug Delivery Systems, using Tetracycline antibiotic as a suitable model drug. The selected nanosponges featured a different composition ratio between the two host co-monomer components, and the possible presence of ionisable amine or carboxyl groups deriving from chemical post-modification. The pH-dependent absorption and release abilities of the materials were verified; in particular release kinetics showed the occurrence of a simple first-order profile. The antibacterial activity of nanosponge-tetracycline composites suitably prepared under sterile conditions was assayed towards both Gram-positive and Gram-negative typical bacterial strains, showing in some cases an interesting improvement of the biocidal activity.

Nanosponges (NS) of etodolac(ETO) was prepared using the emulsion solvent diffusion method ; the effects of drug: polymer ratio, the effect of level concentration of internal phase and stirring time and other variables that effect on the physical characteristics of NS were investigated and characterized, The selected formula was lyophilized then incorporated into hydrogel ; which also evaluated .The results show that the formulation that contain Drug: PVA:EC in ratio 1:3:2 is the best with smallest particle size 40.2±0.098 with polydispersibility0.005 and in vitro release 97.6±0.11%, , ETO NS Carbopol hydrogel produced a significant(p

In recent decades, the rise in the investigation of new drugs had made health-care system expensive compared to conventional drug delivery systems and techniques. The present drug delivery systems have become highly productive and are growing fast. Majority of the anticancer agent has low water solubility resulting in multistep synthetic routes that require higher selectivity and specificity that can cause difficulty in the development of the formulation. Nanosponges (NSs) are branched cyclodextrin (CD) polymeric systems which have proven to be a boon in the pharmaceutical and biomedical fields. Different kinds of NSs based on different types of CDs and crosslinkers are used for developing of new drug formulations from the past few years for various applications in health care. Nanotechnology has overcome the issues regarding the drug solubility, stability, and other parameters and has attained success in achieving of sustained release, increased activity, improved permeability, delivery of nucleoprotein, the stimuli-responsive release of the drug, and improved drug bioavailability. There is a huge eruption of research on NSs for cancer treatment. Multiple anticancer moieties have been developed, taking into account the pharmacological and physicochemical perspective of the drug to develop a NS formulation. Our target in this review is to catch an efficient and far-reaching NSs for malignancy cancer treatment announced until now. This survey will give a perfect stage for providing details for researchers taking a shot at using new polymers for improving the treatment of the disease using nanotechnology. The present article provides details regarding antineoplastic molecules and provides ideas on CD-based NSs specifically using curcumin, tamoxifen, resveratrol, quercetin, oxygen-NSs, temozolomide, doxorubicin, and 5-fluorouracil (5-FU), and erlotinib (ETB) glutathione.

There are many hydrophobic or poorly soluble nutrients and bioactive compounds which are essential for human health, such as phenolic compounds, carotenoids, essential oils, essential fatty acids, and insoluble vitamins. The low bioavailability and sustainability of these compounds are the main challenges for their use in the pharmaceuticae and food industries. Nanoencapsulation can be a favourable approach for protecting hydrophobic food bioactive compounds against unsuitable circumstances and enhance their bioavailability. In this review, several nanoencapsulation delivery systems for hydrophobic compounds, such as inclusion complexes through cyclodextrins, amylose, and yeast cells, nanogels, nanoemulsions, nanofibers, nanosponges, nanoliposomes, and nanoparticles made with lipids and biopolymers are discussed. Also, the toxicity and safety aspects of the nanocarriers loaded with hydrophobic food bioactive compounds has been covered. Different studies on encapsulation of hydrophobic food bioactives have shown that by incorporating them into sophisticated nanocarriers, promising and favourable results can be achieved such improvement in water solubility, antioxidant and other health-promoting properties, in vitro gastrointestinal release profile, and better protection against process and environment harsh conditions such as light, oxygen, high temperatures, humidity, etc.

Purpose Pore-forming toxins (PFTs) perform important functions during bacterial infections. Among various virulence-targeting therapies, nanosponges (NSs) have excellent neutralization effects on multiple PFTs. To enhance treatment efficacy, NSs tend to be incorporated into other biomaterials, such as hydrogels. Methods In the present work, red blood cell (RBC) vesicles were harvested to wrap polymer nanoparticles, leading to the formation of NSs, and the optimal Pluronic F127 hydrogel concentration was determined for gelation. Then, a novel detoxification system was constructed by incorporating NSs into an optimized Pluronic F127 hydrogel (NS-pGel). Next, the system was characterized by rheological and sustained release behavior as well as micromorphology. Then, the in vitro neutralization effect of NS-pGel on various PFTs was examined by a hemolysis protocol. Finally, therapeutic and prophylactic detoxification efficiency was evaluated in a mouse subcutaneous infection model in vivo. Results A thermosensitive, injectable detoxification system was successfully constructed by loading NSs into a 30% Pluronic F127 hydrogel. Characterization results demonstrated that the NS-pGel hybrid system sustained an ideal fluidity and viscosity at lower temperatures but exhibited a quick sol-gel transition capacity near body temperature. In addition, this hybrid system had a sustained release behavior accompanied by good biocompatibility and biodegradability. Finally, the NS-pGel system showed neutralization effects similar to those of NSs both in vitro and in vivo, indicating a good preservation of NS functionality. Conclusion In conclusion, we constructed a novel temperature-sensitive detoxification system with good biocompatibility and biodegradability, which may be applied to the clinical treatment of PFT-induced local lesions and infections., Graphical Abstract

Mycotoxins present a great concern to food safety and security due to their adverse health and socio-economic impacts. The necessity to formulate novel strategies that can mitigate the economic and health effects associated with mycotoxin contamination of food and feed commodities without any impact on public health, quality and nutritional value of food and feed, economy and trade industry become imperative. Various strategies have been adopted to mitigate mycotoxin contamination but often fall short of the required efficacy. One of the promising approaches is the use of bioactive plant components/metabolites synergistically with mycotoxin-absorbing components in order to limit exposure to these toxins and associated negative health effects. In particular, is the fabrication of β-cyclodextrin-based nanosponges encapsulated with bioactive compounds of plant origin to inhibit toxigenic fungi and decontaminate mycotoxins in food and feed without leaving any health and environmental hazard to the consumers. The present paper reviews the use of botanicals extracts and their phytochemicals coupled with β-cyclodextrin-based nanosponge technology to inhibit toxigenic fungal invasion and detoxify mycotoxins., Food Science; Food Safety; Mycotoxin; Fungal invasion; Detoxification; Plant extracts; Nanosponge; Food and Feed.

Nanoparticles cloaked in human lung and immune cell membranes act as decoys to neutralize SARS-CoV-2 in cell culture, preventing host cell infection.

Cyclodextrin-based nanosponges have been found to be promising drug delivery systems. This paper investigates an application that still needs to be studied in depth, that is, the oral delivery of peptides and proteins, choosing insulin as a case study. The nanosponge was synthesized by crosslinking β-cyclodextrins with pyromellitic dianhydride, adopting a top-down approach for its subsequent formulation. A physicochemical characterization, in-vitro and in-vivo tests were carried out on the formulation developed. It was nanometric (around 250 nm) with high negative zeta potential, mucoadhesion and swelling properties, good loading capability (about 14%) and encapsulation efficiency (above 90%). The in-vitro release of insulin was negligible at a gastric pH (below 2%) while sustained at an intestinal pH, thus showing a pH-sensitive behaviour of the nanosponge. The Caco-2 cell permeability assay proved that the intestinal permeation of insulin was enhanced when loaded inside the nanosponge. The in-vivo studies confirmed the presence of insulin in rat plasma and a marked hypoglycemic effect in diabetic mice after duodenal and oral administrations, respectively. These preliminary results are encouraging with a view to continuing to study this β-cyclodextrin nanosponge technology for the oral administration of insulin and extending this approach to other proteins of pharmaceutical interest.

The design and structural optimisation of a novel polysaccharide-based nanomaterial for the controlled and sustained release of doxorubicin are here reported. A cross-linked polymer was obtained by reacting a tetraglucose, named cyclic nigerosyl-1-6-nigerose (CNN), with pyromellitic dianhydride. The cross-linking reaction formed solid nanoparticles, named nanosponges, able to swell as a function of the pH. Nanoparticle sizes were reduced using High Pressure Homogenization, to obtain uniform nanosuspensions. Doxorubicin was incorporated into the CNN-nanosponges in a good extent. DSC and solid state NMR analyses proved the drug interaction with the polymer matrix. In vitro studies demonstrated pH-dependent slow and prolonged release kinetics of the drug from the nanoformulation. Doxorubicin-loaded CNN-nanosponges were easily internalized in A2780 cell line. They might considered an intracellular doxorubicin reservoir, able to slowly release the drug over time. CNN-nanosponges may be promising biocompatible nanocarriers for the sustained delivery of doxorubicin with potential localised application in cancer treatments.

The aim of this study was to explore the feasibility of complexing the poorly water-soluble drug atorvastatin calcium (AC) with β-cyclodextrin (β-CD) based nanosponges (NS), which offer advantages of improving dissolution rate and eventually oral bioavailability. Blank NS were fabricated at first by reacting β-CD with the cross-linker carbonyldiimidazole at different molar ratios (1:2, 1:4, and 1:8), then NS of highest solubilization extent for AC were complexed with AC. AC loaded NS (AC-NS) were characterized for various physicochemical properties. Pharmacokinetic, pharmacodynamics and histological finding of AC-NS were performed in rats. The prepared AC-NS showed particles size ranged from 408.7 ± 12.9 to 423 ± 15.9 nm while zeta potential values varied from -21.7 ± 0.90 to -22.7 ± 0.85 mV. The loading capacity varied from 17.9 ± 1.21 to 34.1 ± 1.16%. DSC, FT-IR, and PXRD studies confirmed the complexation of AC with NS and amorphous state of the drug in the complex. AC-NS displayed a biphasic release pattern with increase in the dissolution rate of AC as compared to plain AC. Oral administration of AC-NS (1:4 w/w, drug: NS) to rats led to 2.13-folds increase in the bioavailability as compared to AC suspension. Pharmacodynamics studies in rats with fatty liver revealed significant reduction (p .05) in total cholesterol, triglyceride, LDL-C and increased level of beneficial HDL-C along with improvement in the associated liver steatosis as confirmed through photomicrographs of liver sections. In this study, we confirmed that complexation of AC with NS would be a viable approach for improving oral bioavailability and in vivo performance of AC.

The objective of the present study was to produce extended release nateglinide nanosponges for oral delivery. Preparation of nanosponges leads to solubility enhancement. Nateglinide is a BCS Class II drug, having low solubility. So, to increase the solubility of nateglinide it is formulated into nanosponges. Nanosponges using ethyl cellulose as a polymer and dichloromethane as a cross-linker were prepared successfully by ultra-sound assisted synthesis method. The effects of different drug: placebo ratios on the physical characteristics of the nanosponges as well as the drug content and in vitro drug release of the nanosponges were investigated. Particle size analysis and surface morphology of nanosponges were performed. The scanning and transmission electron microscopy of nanosponges showed that they were spongy in nature. The particle size was found to be in the range 46.37 - 97.23 nm out of which particle size of the optimized formulation was 51.79 nm and the drug content was found to 79.43 %. The optimized nanosponge formulations were selected for preparing nanosponge tablets for extended drug delivery by oral route. These tablets were prepared using xanthan gum and PVP K-30 and were evaluated by pre-compression and post-compression parameters. The nateglinide nanosponges tablet formulation were studied for different parameters using Design Expert Software. All formulations were evaluated for in vitro drug release analyzed according to various release kinetic models and it was found that it follows zero order release kinetics.

Cyclodextrin-based nanosponges (CD-NS) are innovative cross-linked cyclodextrin polymers nanostructured within three-dimensional network. CD-NS are highly porous nanoparticles characterized by crystalline or amorphous structure, spherical shape and swelling properties. Different cross-linkers provide variety of nanosponges. The polarity, dimension of the polymer mesh and release of entrapped molecule can be easily tuned by varying the type of cross-linker and degree of cross-linking. The site-specific targeting can be achieved by conjugating various ligands on the surface of nanosponge. They offer unique advantage of controlled release and are biologically safe and biodegradable material. Cyclodextrin-based nanosponges can form complexes with different types of lipophilic or hydrophilic molecules. The nanosponges could be used to improve the aqueous solubility of poorly water-soluble molecules, protect degradable substances and as innovative carrier in pharmaceuticals, cosmetics, protein/peptide delivery, diagnostics, enzyme-catalysed reactions, environmental control and agrochemistry.

This brief communication appraises nanosponges regarding their potential application in drug industry. Initiating from their basics, their particular characteristics are briefed. Apart from this, one of the very recent application of nanosponges is outlined along with future perspectives.

The inclusion of polyphenols into nanoporous materials may significantly improve their application as radical trapping agents for therapeutic purposes. In the present work, nanosponges based on hypercross- linked cyclodextrins and calixarenes (NS1–NS3) were used as carriers of three natural phenolic antioxidants: quercetin (Que), curcumin (Cur) and phenethyl caffeate (Phec). Good w/w loadings, namely 7.3% for the Que–NS1 composite, 17.3% for Cur–NS2 and 12.9% for Phec–NS3, were achieved. The release kinetics and the inhibition rate constants (kinh) of the reaction with alkylperoxyl radicals (ROO.) in 0.1 M phosphate buffer solutions at pH 7.4 were studied and indicated better antioxidant activity as compared to the phenols alone. The three phenols suffered a dramatic reduction of kinh upon increasing their concentration, as a result of their degradation. The inclusion into the nanosponges protected the antioxidants and provided a controlled release in an aqueous medium. Hence, different applications can be envisaged, in food and pharmaceutical technology fields.

Psoriatic arthritis is a chronic inflammatory joint disease which is one of the types of psoriasis. 25% of all psoriasis patients develop psoriatic arthritis. It is characterised with innate and adaptive immune responses. The main objective of the present work was to prepare characterization and evaluate the Celecoxib nanosponges for the treatment of Psoriatic Arthritis. It is a non-steroidal anti-inflammatory drug (NSAID) having low solubility and low bioavailability. In order to increase the solubility, this drug was incorporate in nanosponges by melting technique. The prepared formulation was evaluated for different parameters. SEM images confirm that the prepared formulation was spherical and porous in nature. Particle size analysis shows that as the cross-linker ratio increases, there is increase in the particle size of nanosponges. Particle size was in the size range of 201.69 nm. The in vitro studies were carried out for prepared nanosponges which showed drug release of 89.69% in 24 h. Keywords: Nanosponges, Psoriatic arthritis, NSAID, Drug release

The background behind the delivery of drugs topically is to render localized action on the skin. Topical drug delivery employing conventional formulations such as ointment, creams suffers with lower uptake of drug due to its hydrophobic nature eventually leads to ineffective treatment. To overcome these issues, topical delivery of β-cyclodextrin-based nanosponges has opted, that facilitates the controlled drug release over a period of time. Topical drug delivery is an intriguing and persuading access to treat skin related infections/diseases owing to their lower risk of reactions a the systemic level duly contrasted with oral or parenteral drug administration and high drug level can be accomplished at the site of ailment. β-Cyclodextrin nanosponges (NS) are composed of permeable nanostructure material comprising of hyper cross-linked β-cyclodextrin system, ensures enhancement in solubility, provides desirable controlled release wider range of drugs by forming inclusion complexes, which diminish the recurrence portion of drug and maintain a distance from systemic absorption. Ketoconazole, an antifungal agent classified as BCS II, used to treat fungal infections and candidiasis. The stumbling block in attaining the effective therapeutic application and efficacy of ketoconazole is due to its moderate lipid solubility (Log P 4.35).

This study investigated the effects of free paclitaxel (PTX) and PTX-loaded in pyromellitic nanosponges (PTX-PNS) in reducing in vitro and in vivo melanoma cell growth and invasivity, and in inhibiting angiogenesis. To test the response of cells to the two PTX formulations, the cell viability was evaluated by MTT assay in seven continuous cell lines, in primary melanoma cells, both in 2D and 3D cultures, and in human umbilical vein endothelial cells (HUVECs) after exposure to different concentrations of PTX or PTX-PNS. Cell motility was assessed by a scratch assay or Boyden chamber assay, evaluating cell migration in presence or absence of diverse concentrations of PTX or PTX-PNS. The effect of PTX and PTX-PNS on angiogenesis was evaluated as endothelial tube formation assay, a test able to estimate the formation of three-dimensional vessels in vitro. To assess the anticancer effect of PTX and PTX-PNS in in vivo experiments, the two drug formulations were tested in a melanoma mouse model obtained by B16-BL6 cell implantation in C57/BL6 mice. Results obtained were as follows: 1) MTT analysis revealed that cell proliferation was more affected by PTX-PNS than by PTX in all tested cell lines, in both 2D and 3D cultures; 2) the analysis of the cell migration showed that PTX-PNS acted at very lower concentrations than PTX; 3) tube formation assay showed that PTX-PNS were more effective in inhibiting tube formation than free PTX; and 4) in vivo experiments demonstrated that tumor weights, volumes, and growth were significantly reduced by PTX-PNS treatment with respect to PTX; the angiogenesis and the cell proliferation, detected in the tumor samples with CD31 and Ki-67 antibodies, respectively, indicated that, in the PTX-PNS-treated tumors, the tube formation was inhibited, and a low amount of proliferating cells was present. Taken together, our data demonstrated that our new PTX nanoformulation can respond to some important issues related to PTX treatment, lowering the anti-tumor effective doses and increasing the effectiveness in inhibiting melanoma growth in vivo.

The lack of pharmaceutical antidotes for deadly toxicants has motivated tremendous research interests in seeking synthetic nanoscavengers to absorb and neutralize harmful biological or chemical agents. Herein, we report a cell-membrane-cloaked oil nanosponge formulation capable of dual-modal detoxification. The biomimetic oil nanosponge consists of an olive oil nanodroplet wrapped by a red blood cell membrane. In such a construct, the oil core can nonspecifically soak up toxicants through physical partition and the cell membrane shell can specifically absorb and neutralize toxicants through biological binding. The dual-modal detoxification capability of the oil nanosponges was validated using three distinct organophosphates (OPs), including paraoxon, diisopropyl fluorophosphate, and dichlorvos. By inhibiting acetylcholinesterase, OPs cause the accumulation of acetylcholine, which leads to neuromuscular disorders and even death. In mouse models of OP poisoning, the oil nanosponges reduced clinical signs of OP intoxication, lowered OP concentration in tissues, and greatly enhanced mouse survival in both the therapeutic regimen and the prophylactic regimen. Overall, oil nanosponges combine the merits of both cell membrane and oil nanodroplets for safe and effective detoxification, which also serve as a prototype of multimodal detoxification platforms.