Nanogel Formulations Research Articles

Bilastine-Loaded Transethosome Based Nanogel for the Treatment of Allergic Reactions: An In vitro Characterization

Objective: The goal of the current study was to formulate and evaluate bilastine-loaded transethosomal nanogel. Bilastine has 60% oral bioavailability, which restricts the rate of absorption and dissolution and classifies it under BCS class II drugs, which can be overcome by incorporating bilastine in transethosomal nanogel formulation in the treatment of urticaria. Methods: Bilastine-loaded transethosomes were prepared using a thin film hydration method with different proportions of Tween 80 and ethanol by using a rotary evaporator and incorporated into a transethosomal gel using Carbopol 934 as a polymer by dispersion method. Results: The bilastine-loaded transethosomal formulation was optimized by using the “Box Behnken design” and evaluated for various parameters. The optimized formulation was found to be stable, as determined by the zeta potential of −27.0 mV and polydispersity index (PDI) of 0.167, and vesicle size was found to be 183nm and exhibiting the maximum entrapment efficiency of up to 80.23%. The drug content of the transethosomal gel was found to be 81.56%. The best results were obtained with a transethosomal gel prepared with 1% Carbopol 934 (TF7G2). The optimized batch showed prolonged in-vitro release of bilastine for 8 hrs. Ex vivo skin permeation studies showed 76.23 ± 2.63% permeation in comparison with plain gel. Conclusion: Transethosomal nanogel batches were optimized based on drug content, viscosity, uniformity of drug content, zeta potential, spreadability, pH, drug release, and stability testing, exhibiting good results. The results of this investigation showed that the transethosomal nanogel loaded with bilastine might be used to improve bilastine delivery through the skin with greater bioavailability.

Formulation and Evaluation of Different Nanogels of Tapinarof for Treatment of Psoriasis.

Psoriasis is an immune-mediated skin condition. There are many therapeutic options for its treatment; however, none of them is completely effective. Tapinarof is a promising new active substance; it was recently approved by the FDA for the treatment of psoriasis. The aim of our study was to prepare topical nanoformulations of the active substance to improve its bioavailability and therapeutic effect. The biocompatibility investigation of the formulations was carried out by MTT assay, and the size distribution of the preparations was investigated by DLS. In parallel, the rheological properties and the texture were examined, and the in vitro release of tapinarof was assessed by the Franz diffusion method. An in vitro wound healing assay was also carried out to study the drug's properties. Our results show that the preparations were safe on HaCaT cells. The particle size of the formulations was proven to be in the nanoscale range. In the in vitro release studies, nanogel II. showed greater release of the active substance. According to the wound healing assay, incorporation of the drug into nanoformulations increases the antiproliferative and antimigration activity of the drug. Overall, nanoformulations of tapinarof were successfully prepared, and our results suggest that they can be a useful addition to the current therapeutic practice of psoriasis.

Development and Characterization of Oxiconazole Loaded Plga Nanogel.

The goal of the current study is to develop and improve polylactic co-glycolic acid (PLGA) loaded with oxiconazole nanogel for topical application. Oxiconazole Nanoprecipitation was used to create the nanoparticles method using PLGA and acetone. The point prediction method served as the foundation for the ideal oxiconazole nanoparticle composition using the Minitab®21 software, three levels two factors (32 ). The optimized composition of oxiconazole nanoparticle showed a particle size of 185 ± 0.5nm with an entrapment efficiency of 95.2 ± 0.09%. Using chitosan, a naturally occurring polymer, the ideal oxiconazole nanoparticle composition was further transformed into a gel formulation. The developed topical nano gel formulation underwent additional evaluations for antifungal, drug release, permeability, and nano gel characterization. The developed oxiconazole nanogel formulation had the ideal drug content, pH, viscosity, and spreadability. The results of the medication release and penetration investigation showed that Oxiconazole released slowly (74.06 ± 0.5%) with significantly enhanced permeation across Franz diffusion cell using membrane. The antifungal ex-vivo study and skin irritancy study of nanogel results would conclude higher activity of oxiconazole nano gel. According to the overall analysis of the data, oxiconazole nanogel is the best delivery method for treating fungal infections on the skin.

A Nanogel Formulation of Anti-VEGF Peptide for Ocular Neovascularization Treatment.

Age-related macular degeneration (AMD) is an eye disorder that can lead to visual impairment in elder patients, and current treatments include repeated injections of monoclonal antibody-based antivascular endothelial growth factor (anti-VEGF) agents. This study investigates the potential of a nanoformulation of a peptide anti-VEGF molecule for neovascular AMD. Anti-VEGF peptide HRHTKQRHTALH (HRH), which has high affinity to VEGF-Fc receptor, was used as the bioactive agent to control neovascularization of the retina. The nanoformulation consisting of hyaluronic acid nanogel was generated by incorporating divinyl sulfone and cholesterol to increase the stability and control the size of the nanodrug. The encapsulation efficacy of nanogel was 65%, and drug release was 34.72% at the end of 192 h. Obtained nanogels were efficiently internalized in 15 min by human umbilical vascular endothelial cells (HUVECs) and ARPE-19 cells, and results indicate that nanoformulation is not toxic to ARPE-19 cells, whereas it inhibits HUVEC proliferation owing to anti-VEGF peptide in the nanogel structure. In the coculture experiment in which retinal penetration was modeled, it was observed that the nanogel reached HUVECs and negatively affected their proliferation without disturbing the monolayer of ARPE-19 cells. In vivo experiments with chick chorioallantoic membrane revealed that nanogel formulation has higher antiangiogenesis activity compared to free HRH. Additionally, in an oxygen-induced retinopathy model, the excessive growth of blood vessels was notably suppressed in mice treated with HRH-loaded nanogel. This research indicates that nanogels formulated in this study are promising candidates as a topical treatment for AMD.

Leukemia Cell Hitchhiking Hypoxia Responsive Nanogel for Improved Immunotherapy of Acute Myeloid Leukemia

AbstractImmune checkpoint blockade (ICB) with anti‐CD47 antibodies (aCD47) is a promising therapeutic approach that has the potential to revolutionize the treatment of acute myeloid leukemia (AML). However, the low immune response rate and high systemic hematotoxicity remain substantial barriers to its success in clinical AML treatment. A synthetic protein nanogel formulation of aCD47 and resiquimod (R848) (termed CR‐TNG) is developed that targets TIM‐3 on the surface of leukemia cells. Upon intravenous injection, the CR‐TNG efficiently conjugates onto the blood‐circulating leukemia cells and migrates toward the bone marrow (BM) by exploiting the natural BM homing capability of leukemia cells. CR‐TNG releases aCD47 and R848 in a bone marrow hypoxic microenvironment, which significantly induces immunosuppression and enhances the anti‐leukemia immune response by activating macrophage “eat me” signaling and priming myeloid macrophages in the BM niche. These findings provide a leukemia cell‐hitchhiking drug delivery strategy that addresses both systemic hematotoxicity and low immune response rate in AML.

PH-Sensitive Fluorescent Probe in Nanogel Particles as Theragnostic Agent for Imaging and Elimination of Latent Bacterial Cells Residing Inside Macrophages.

Rhodamine 6G (R6G) and 4-nitro-2,1,3-benzoxadiazole (NBD) linked through a spacer molecule spermidine (spd), R6G-spd-NBD, produces a fluorescent probe with pH-sensitive FRET (Förster (fluorescence) resonance energy transfer) effect that can be useful in a variety of diagnostic applications. Specifically, cancer cells can be spotted due to a local decrease in pH (Warburg effect). In this research, we applied this approach to intracellular infectious diseases-namely, leishmaniasis, brucellosis, and tuberculosis, difficult to treat because of their localization inside macrophages. R6G-spd-NBD offers an opportunity to detect such bacteria and potentially deliver therapeutic targets to treat them. The nanogel formulation of the R6G-spd-NBD probe (nanoparticles based on chitosan or heparin grafted with lipoic acid residues, Chit-LA and Hep-LA) was obtained to improve the pH sensitivity in the desired pH range (5.5-7.5), providing selective visualization and targeting of bacterial cells, thereby enhancing the capabilities of CLSM (confocal laser scanning microscopy) imaging. According to AFM (atomic force microscopy) data, nanogel particles containing R6G-spd-NBD of compact structure and spherical shape are formed, with a diameter of 70-100 nm. The nanogel formulation of the R6G-spd-NBD further improves absorption and penetration into bacteria, including those located inside macrophages. Due to the negative charge of the bacteria surface, the absorption of positively charged R6G-spd-NBD, and even more so in the chitosan derivatives' nanogel particles, is pronounced. Additionally, with a pH-sensitive R6G-spd-NBD fluorescent probe, the macrophages' lysosomes can be easily distinguished due to their acidic pH environment. CLSM was used to visualize samples of macrophage cells containing absorbed bacteria. The created nanoparticles showed a significant selectivity to model E. coli vs. Lactobacillus bacterial cells, and the R6G-spd-NBD agent, being a mild bactericide, cleared over 50% E.coli in conditions where Lactobacillus remained almost unaffected. Taken together, our data indicate that R6G-spd-NBD, as well as similar compounds, can have value not only for diagnostic, but also for theranostic applications.

Facile‐Prepared Size‐Controllable Nanogels for Enhancing Bidirectional Translocation, Control Efficiency, and Security of Nanopesticide

AbstractNanopesticides have been acknowledged by International Union of Pure and Applied Chemistry as a critical tool for revolutionizing future agricultural practices. However, the existing nanopesticides are often plagued by high costs, strict preparation conditions, uncontrollable size, and poor stability. Herein, taking the non‐systemic insecticide lambda‐cyhalothrin (LC) as a model pesticide, a series of LC‐loaded poly(octyl acrylate) nanogel formulations (LONFs) simultaneously featuring easy‐preparation, size‐controllable, and targeted delivery using microemulsion polymerization are developed. By adjusting the ratio of surfactants, the size of LONFs can be accurately designed to be 20, 50, 100, and 200 nm, exhibiting good stability under unconventional storage conditions (0 °C, 54 °C, ultraviolet radiation). Furthermore, reducing the particle diameter enhances the bidirectional translocation of LONFs in Vicia faba L., potentially reaching an optimal diameter (≈20 nm) for unique and rapid transport. LONFs increase the acute toxicity of LC to Aphis craccivora compared to conventional microemulsions (with a maximum reduction of 82.40% in LC50 at 24 h). Additionally, LONFs alter the lethal process of LC in human embryonic kidney 293T cells, with minimal cytotoxicity at a concentration of general application (40 mg L−1). This strategy simultaneously considers convenience, size controllability, and efficiency, providing a feasible method for the industrial development of nanopesticides.

Aktivitas Antioksidan Formula Nano Gel Kombinasi Daun Sonneratia caseolaris dan Trigona sp. Propolis

Sonneratia caseolaris and Kelulut propolis (Trigona sp.) are used by people to protect the face from sun exposure. Both have antioxidant potential, but until now no one has used the combination of these two natural ingredients as an antioxidant. The aims of this research were to obtain antioxidant activity from nano gel formula combination of Sonneratia caseolaris and Trigona sp Propolis extracts. The nano gel formulation was made into 3 formulations with concentrations of F1 (1:1), F2 (1:2) and F3 (2:1) by evaluating the preparation and antioxidant activity by using DPPH method. The evaluation results showed that all of the nano gel formulas were in accordance with the standard characteristics of the preparation and strong antioxidant activities with IC50 (µg/mL) result : F1 (17.568), F2 (35.112) and F3 (14.503). Based on the IC50 results, the greatest antioxidant activity was obtained in Formula 1.

Curcumin Nanogel Preparations: A Promising Alternative for Psoriasis Treatment.

Curcumin is a naturally occurring polyphenolic compound extracted from the rhizomes of Curcuma longa, commonly known as turmeric. It has been used for centuries in traditional medicine and is gaining increasing attention in modern medicine owing to its potential therapeutic benefits. Psoriasis is a chronic inflammatory disease characterized by red scaly patches on the skin. Curcumin has been found to be effective in treating psoriasis by inhibiting the activity of various enzymes and proteins involved in the inflammation and proliferation of psoriatic skin cells. Nanogel preparation of curcumin has been found to be a promising approach for the delivery of compounds to treat psoriasis. Nanogels are composed of biocompatible and biodegradable crosslinked hydrogels. The nanogel formulation of curcumin increases its solubility, stability, and bioavailability, indicating that a lower dose is needed to achieve the same therapeutic effect. This review article suggests that the nanogel preparation of curcumin can be a better alternative for psoriasis treatment as it increases the bioavailability and stability of curcumin and also reduces the required dosage. This study suggests that curcumin nanogel preparations are promising alternatives to traditional psoriasis treatments and could potentially be used as a more effective and safe treatment option. This article highlights the need for further research to fully understand the potential of curcumin nanogel preparations for psoriasis treatment in humans.

Pongamia pinnata seed extract-mediated green synthesis of silver nanoparticle loaded nanogel for estimation of their antipsoriatic properties.

This research describes the eco-friendly green synthesis of silver nanoparticles employing Pongamia pinnata seed extracts loaded with nanogel formulations (AgNPs CUD NG) to improve the retention, accumulation, and the penetration of AgNPs into the epidermal layer of psoriasis. AgNPs were synthesized using the Box-Behnken design. Optimized AgNPs and AgNPs CUD NG were physico-chemically evaluated using UV-vis spectroscopy, SEM, FT-IR, PXRD, viscosity, spreadability, and retention studies. It was also functionally assessed using an imiquimod-induced rat model. The entrapment efficiency of AgNPs revealed ~ 79.35%. Physico-chemical parameters announced the formation of AgNPs via surface plasmon resonance and interaction between O-H, C = O, and amide I carbonyl group of protein extract and AgNO3. Optimized AgNPs showed spherical NPs ~ 116nm with better physical stability and suitability for transdermal applications. AgNPs CUD NG revealed non-Newtonian, higher spreadability, and better extrudability, indicating its suitability for a transdermal route. AgNPs CUD NG enhanced the retention of AgNPs on the psoriatic skin compared to normal skin. Optimized formulations exhibit no irritation by the end of 72h, indicating formulation safety. AgNPs CUD NG at a dose of 1 FTU showed significant recovery from psoriasis with a PASI score of ~ 0.8 compared to NG base and marketed formulations. Results indicated that seed extract-assisted AgNPs in association with CUD-based NG formulations could be a promising nanocarrier for psoriasis and other skin disorders.

Karanjin-loaded soya lecithin-based ethosomal nanogel for the therapeutic intervention of psoriasis: formulation development, factorial design based-optimization, in vitro and in vivo assessment

This study aimed to develop and optimize karanjin-loaded ethosomal nanogel formulation and evaluate its efficacy in alleviating symptoms of psoriasis in an animal model induced by imiquimod. These karanjin-loaded ethosomal nanogel, were formulated to enhance drug penetration into the skin and its epidermal retention. Karanjin was taken to formulate ethosomes due to its potential ani-psoriatic activity. Ethosomes were formulated using the cold method using 32 full factorial designs to optimize the formulation components. 9 batches were prepared using two independent variables X 1: concentration of ethanol and X 2: concentration of phospholipid whereas vesicle size (Y 1) and percentage entrapment efficiency (Y 2) were selected as dependent variables. All the dependent variables were found to be statistically significant. The optimized ethosomal suspension (B3) exhibited a vesicle size of 334 ± 2.89 nm with an entrapment efficiency of 94.88 ± 1.24% and showed good stability. The morphology of vesicles appeared spherical with smooth surfaces through transmission electron microscopy analysis. X-ray diffraction analysis confirmed that the drug existed in an amorphous state within the ethosomal formulation. The optimized ethosome was incorporated into carbopol 934 to develop nanogel for easy application on the skin. The nanogel underwent characterization for various parameters including spreadability, viscosity, pH, extrudability, and percentage drug content. The ethosomal formulation remarkably enhanced the skin permeation of karanjin and increased epidermal retention of the drug in psoriatic skin compared to marketed preparation and pure drug. A skin retention study showed that ethosomal nanogel formulation has 48.33% epidermal retention in 6 h. In vivo, the anti-psoriatic activity of karanjin ethosomal nanogel demonstrated significant improvement in psoriasis, indicated by a gradual decrease in skin thickness and scaling as reflected in the Psoriasis Severity Index grading. Therefore, the prepared ethosomal nanogel is a potential vehicle for improved topical delivery of karanjin for better treatment of psoriasis.

Revolutionizing Arthritis Care: Cutting-Edge Nanogel Formulations for Targeted, Long-Lasting Relief and Enhanced Mobility

Arthritis, which impacts individuals all over the globe, is characterized by severe pain and a high prevalence rate. Current treatments for the illness come with a number of obstacles and difficulties. It is necessary to explore alternative paradigms, as systemic medications aren’t necessarily the greatest choice. The new discipline of nanotechnology has the potential to significantly alter several aspects of arthritis treatment. Therefore, the work provides strong support for developing novel therapies employing compositions of topical nanogels. Traditional systemic narcotics have their limitations, and the evolution of arthritis treatments has to take that into consideration. Thus, novel nanogel formulations offered as a nanotechnology solution may out to be quite advantageous. Applying nanogels to product design has been a significant administrative step. Nanogels offer unparalleled precision and efficiency, whether you’re dealing with simple concepts, cutting-edge techniques for surface modification, or intricate strategies for drug encapsulation. New data from pain evaluations, clinical studies, and comparisons to traditional therapies have supported their revolutionary potential and effectiveness. However, the patient’s health must always come first. While we strive to mitigate adverse effects and evaluate long-term ramifications, the positive outcomes of our biocompatibility testing offer reassurance regarding the safety profile of nanogels. For regulatory and ethical considerations, there must be transparency, informed permission, and equitable access for nanotechnology-powered arthritic treatments. This study calls for additional research into the use of nanotechnology in the treatment of arthritis because recent advances in nanogel technology have the ability to completely transform the current approach to treating this debilitating disease, bringing about a new era of precision medicine.

Development of topical silver nano gel formulation of Bixin: Characterization, and evaluation of anticancer activity

ObjectiveSkin cancer refers to the pathological condition characterized by the proliferation of atypical skin cells in an uncontrolled manner. Plant-based products such as bixin although show promising anticancer properties, but maintaining their stability in a formulation is a difficult task. The objective of the research is to formulate a silver nanoparticle gel preparation of bixin and evaluate its anticancer properties. MethodsThe extract from Bixa orellana seed was prepared by hot extraction technique to isolate the active ingredient, bixin. A green synthesis approach was utilized for preparing the silver nanoparticle gel of bixin (BOAgNPs). Characterization of silver nanoparticles was done using FTIR, scanning electron microscopy, compatibility study, homogeneity testing, pH evaluation, and drug content determination. The in-vitro anticancer activity was performed using cell lines (B16F10) and in-vivo by chemical carcinogen (7,12-dimethylbenz (a) anthracene) in mice. ResultsThe BOAgNPs-loaded topical gel was found to be homogeneous (clear orange color) and pH-compatible (pH ≈ 6.66) with the skin. The characterization studies indicated the presence of all functional groups in the formulation. An optimized batch of bixin-nano gel showed about 60% inhibitory effects on B16F10 cell lines (in-vitro activity) when equated with a reference drug, 5-fluorouracil. The in-vivo anticancer study suggested suppression of tumorigenesis and promotion of the healing process with bixin-nano gel application on the skin. ConclusionThe results suggested the promising anticancer property of bixin when formulated in silver nanoparticle gel. The preparation of silver particles nano gel with bixin might provide an effective alternative option for treating skin cancers, provided more research complements the findings of the present study.

Crosslinked PVA-g-poly(AMPS) Nanogels for Enhanced Solubility and Dissolution of Ticagrelor: Synthesis, Characterization, and Toxicity Evaluation.

In this study, we synthesized PVA-g-poly(AMPS) nanogels with the aim of enhancing the solubility and dissolution of ticagrelor (TGR). Ticagrelor, a noncompetitive, reversible P2Y12 receptor antagonist, is prescribed to treat acute coronary syndrome. Ticagrelor has restricted oral bioavailability (≈36%) because of its poor solubility and permeability. The free radical polymerization methodology was employed to synthesize nanogels with varied concentrations of poly(vinyl alcohol) (polymer), 2-acrylamido-2-methylpropanesulfonic acid (monomer), and N,N-methylene bis(acrylamide) (crosslinker). The prepared nanogels were analyzed by swelling studies, % drug entrapment efficiency (DEE), solubility studies, in vitro drug release studies, zeta sizer, Fourier transform infrared (FTIR) spectroscopy, powder X-ray diffraction (PXRD), thermogravimetric analysis (TGA), differential scanning calorimetry (DSC), and scanning electron microscopy (SEM). The optimized formulation (PA5) revealed a particle size of 45.86 nm, with a polydispersity index (PDI) of 0.41 and a %DEE of 85.1%. FTIR spectroscopy, XRD, and SEM confirmed the formation of crosslinked nanogels with amorphous and porous structures, and TGA/DSC proved their thermal stability. In vitro dissolution studies showed 99.91% drug release, and the ticagrelor solubility from the synthesized formulations was significantly improved up to 8.2-fold. All formulations followed the Korsmeyer-Peppas model with the Fickian diffusion as the release mechanism. The toxicity studies carried out on rats and the MTT assay on the Caco-2 cell line validated the biocompatibility of the nanogel formulations. The outcomes of the current study led to the conclusion that the PVA-g-poly(AMPS) nanogels synthesized by us could be used as dedicated pharmaceutical delivery systems to achieve enhanced solubility and dissolution of ticagrelor.

Formulation and In Vitro Assessment of Polymeric pH-Responsive Nanogels of Chitosan for Sustained Delivery of Madecassoside.

Madecassoside, a triterpenoid saponin compound mainly isolated from the gotu kola herb (Centella asiatica), shows an extensive range of biological activities, including antiapoptotic, antioxidant, anti-inflammatory, moisturizing, neuroprotective, and wound healing effects. It has been highly used in the management of eczema, skin wounds, and other diseases. Due to poor oral bioavailability, membrane permeability, and intestinal absorption, the clinical application of the madecassoside is limited. Hence, a drug carrier system is needed that not only sustains the release of the madecassoside but also overcomes the drawbacks associated with its administration. Therefore, the authors prepared novel pH-responsive chitosan-based nanogels for the sustained release of madecassoside. Free radical polymerization technique was used for cross-linking of polymer chitosan and monomer methacrylic acid in the presence of cross-linker N',N'-methylene bis(acrylamide). The decrease in polymer crystallinity after polymerization and development of nanogels was demonstrated by XRD and FTIR analysis. The effects of nanogel contents on polymer volume, sol-gel analysis, swelling, drug loading, and release were investigated. Results indicated that high swelling and maximum release of the drug occurred at pH 7.4 compared to pH 1.2 and 4.6, indicating the excellent pH-sensitive nature of the engineered nanogels. High swelling and drug release were perceived with the integration of a high quantity of chitosan, while a decline was observed with the high integration of N',N'-methylene bis(acrylamide) and methacrylic acid contents. The same effects of nanogel contents were shown for drug loading too. Sol fraction was reduced, while gel fraction was enhanced by increasing the chitosan load, N',N'-methylene bis(acrylamide), and methacrylic acid. The Korsmeyer-Peppas model of kinetics was trailed by all nanogel formulations with non-Fickian diffusion. The results demonstrated that prepared nanogels can be employed for sustained release of the madecassoside.

Fabrication and evaluation of cross-linked nanogels of Dexibuprofen

The objective of this study was to design and develop an Agarose-based polymeric nanogel network system for solubility enhancement of a lipophilic drug, Dexibuprofen. Polymeric nanogels were synthesized through free radical polymerization where Agarose was cross-linked with 2-Acrylamido-2-methylpropane sulfonic acid (AMPS) in the presence of ammonium persulfate (APS) as an initiator and N, N’-Methylenebisacrylamide (MBA) as crosslinking agent. The resulting polymeric nanogels underwent a comprehensive characterization process including Fourier transform infrared (FTIR), particle size analysis, scanning electron microscopy (SEM), differential scanning calorimetry (DSC), thermal gravimetric analysis (TGA), powder X-ray diffraction (PXRD), and swelling studies to confirm the preparation of a stable polymeric nanogel system. FTIR spectral findings revealed that Agarose was chemically cross-linked with AMPS and confirmed the successful insertion of AMPS chains on the Agarose backbone. Particle size analysis revealed a diameter of 168 nm with a zeta potential of −9.91 mV, providing assurance of a stable polymeric nanogel system. SEM images depicted a highly porous surface. DSC and TGA results showed a more thermally stable network system than individual ingredients. Swelling studies revealed an increased swelling ratio of polymeric nanogels at phosphate buffer of pH 6.8 than acidic buffer of pH 1.2. Dexibuprofen was efficiently loaded into a polymeric nanogel system with a high entrapment efficiency of up to 80%. The solubility of the drug was enhanced when introduced to a polymeric nanogel formulation when compared to pure drug. The system reproducibility was evaluated through in vitro drug release and kinetic modeling of drug release. Toxicity studies confirmed the formulation’s effectiveness, showcasing the developed polymeric nanogels as a promising option for delivering lipophilic drugs, with outstanding physicochemical properties, improved solubility, and minimal oral toxicity.

THE EFFECTIVENESS OF VARIOUS CITRONELLA OIL NANOGEL FORMULATIONS AS A REPELLENT OF AEDES AEGYPTI MOSQUITO

Objective: The aim of this research is to determine the effectiveness of the repellency of various citronella oil nanogel formulations against Aedes aegypti mosquito bites applied to guinea pigs. Methods: The Citronella oil nanogel was prepared by emulsification technique combined with gelling formation. The nanoemulsion formula consists of 6% Citronella oil, 10% propylene glycol, 6% combination of Tween 80 and Span 80 in variation to 4 formula, and deionized water until 100%. Nanoemulsions were then added to the gel base which is composed of Carbopol 940 and TEA. The nanogel formed was characterized physically and its effectiveness against Aedes aegypti mosquito using guinea pigs as an animal model. The repellent activity was determined by the amount of mosquito bites on the guinea pigs’s skin. Results: The organoleptic test displayed that all formulas comply with the requirements, except formula 1. The formula 2, 3, and 4 have particle size below 100 nm and the polydispersity index (PDI) less than 0.5. According to the repellent assay showed that all formulas have the effectiveness much higher than without the intervention. Formula 3 has the highest effectiveness of repellent activity against Aedes aedgypti in guinea pigs’ skin. The repellent activity of Formula 3 showed a significant difference (p-value of 0.005) as compared to nanogel without Citronella oil. Conclusion: The protective power of Citronella oil nanogel Formula 3 is the most effective as compared to the other formula.

Formulation of Lipid Nanoparticles based Nanogel of Sertaconazole Nitrate and its Evaluation

Background: Sertaconazole nitrate is a topical antifungal drug used to treat interdigital tinea pedis in patients with immunocompetent conditions. The class of imidazole includes the antifungal medication sertaconazole nitrate. It is available in topical formulations for treating skin infections, including athlete's foot. Solid lipid nanoparticles (SLN) are at the cutting edge of nanotechnology, with several potential uses in drug delivery and research. Because of their unique size-dependent features, lipid nanoparticles hold the promise of novel therapies. Objective: Drug incorporation into nanocarriers creates a new drug delivery prototype that could be employed for drug targeting. The research aims to study the formulation and evaluation of Sertaconazole nitrate solid lipid nanoparticles. The goal behind formulating SLN gel is to provide and maintain therapeutic concentrations of the drug at the target biological site to maximise therapeutic efficacy and minimise side effects. Methods: Sertaconazole Nitrate Solid Lipid Nanoparticles are prepared by using High Pressure Homogenizer to get nanogel formulation as the final formulation and In-vitro drug release using a diffusion apparatus. The prepared SLNs were evaluated in their FTIR studies to determine compatibility between the drug and the excipients; zeta potential indicates the solid lipid nanoparticle was stable, and polydispersity index was used to determine particle size. Result: The results demonstrate that optimised SLN-based Sertaconazole nitrate gel exhibited the best physicochemical properties, including FTIR studies of the drug, excipients, and optimised formulation demonstrate that all are compatible with each other, particle size is less than 200 nm, zeta potential ranging from 12 to -20 mV, and highest entrapment efficiency is 71.48%. Optimised solid lipid nanoparticles showed good in vitro release and antimicrobial results. The main application of SLN large scale-up is possible, and the drug can be effective with less dose incor-poration. Conclusion: In this research work, the proposed plan of work SLN of Sertaconazole Nitrate was formulated successfully. The preliminary identification tests were performed, such as melting point determination, estimation of λmax by UV-visible spectrophotometry and plot of its calibration curve in solvent and buffer system, and FT-IR investigation to confirm the purity and confirmation of medication. High physical stability and drug loading are advantageous to SLN.

Formulation and Optimization of Polyherbal Nanogel for Dermatological Applications

Aim: The aim of the present investigation was to develop a polyherbal nano gel (PHNG) formulation capable of acting as a potential vehicle to deliver polyherbal phytoconstituents topically. Background: Individual herbs, according to Ayurveda, are insufficient to deliver the intended medicinal effect. It will have a better therapeutic impact with less toxicity when it is optimized as multiple herb combinations in a certain ratio. Objective: The objective of this study was to create a polyherbal gel for the delivery of medication from methanolic extracts of Plumbago zeylanica Linn, Datura stramonium Linn, and Argemone mexicana Linn. Material and Methods: The plant parts chosen for this work include methanolic extracts of Plumbago zeylanica stem, Datura stramonium leaves, Argimone Mexicana areal part. The polyherbal-based nanogel was prepared by low energy self-emulsification technique, and was evaluated for pH, viscosity and spreadability, stability, and drug release. The drug release profile of stable nanogel formulations was studied at various time intervals. Furthermore, the prepared nanogel was characterized by zeta-potential, zeta-sizer, and transmission electron microscopy (TEM). Result: Optimized PHNG had particle size and zeta potential of 11.25nm and -25.73 mV respectively. TEM analysis of optimized formulation revealed the spherical shape of particles. Furthermore, the optimized formulation was found to possess higher stability with a maximum extended cumulative release of up to 240 minutes. Conclusion: We have formulated a polyherbal nanogel that can be validated by physiochemical and surface characterization.

Nano-gel formulation of polyphenolic fraction of tobacco stem for wound healing and its inhibitory efficacies against the receptors of chronic wound development

Current investigation deals with the gel formulation of purified polyphenol loaded nanoparticles for enhanced wound healing. Polyphenols purified using column chromatography an were characterized using HPLC in fractions. Silver nanoparticles were characterization using SEM, AFM, TEM, DLS. Cytotoxic effect was checked on L929 (Mouse fibroblast cells). Bioactive loaded nanoparticles were formulated in gel and subjected for physical characterization. Excision wound wistar rat models were established to measure the wound contraction measurement, histopathological studies, and biochemical assays. Docking and Simulation studies were performed to check the binding and stability with receptors progressing the chronic wound. From the column chromatography, B fraction has shown the presence of maximum polyphenolic content and as well as the polyphenol compounds such as quercetin, rutin and tannic acid as confirmed by the HPLC. Synthesize B fraction-AgNP were found to be below 100 nm in size and spherical in shape as per the characterization. No cytotoxic effect was observed on L929 cells treated with B fraction and its nanoparticles. Formulated B fraction-AgNP gel has revealed the better stability and earlier wound contraction, i.e. before the completion of 14 days of topical treatment. Histopathology studies and collagen content has confirmed the re-epithelization in skin wounds. MD simulation revealed the stability with PI3K and AKT. This can be concluded that tobacco stem polyphenol loaded nanoparticles has potent wound healing activity that can be utilized as nano-drug delivery system for suppression of chronic wound development. Communicated by Ramaswamy H. Sarma