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AbstractThe aim of study was to prepared and evaluated rutin-loaded solid-lipid-nanoparticles (Ru-SLNs) gel for treatment of melanoma cells. SLNs were prepared by ultrasonication method through optimisation and evaluated their mean-diameter, PDI, zeta-potential, morphology, entrapment-efficiency, drug-loading, interaction by FTIR, in vitro skin permeation, stability, antioxidant/MTT assay and fluorescence microscopic. Further developed Ru-SLNs was incorporated into gel and characterised their physicochemical properties, drug contents, in vitro diffusion, ex vivo permeation and retention studies in human cadaver skin. Optimised Ru-SLNs batch showed 556.4 ± 2.6 nm mean-diameter, −21.9 mV zeta-potential, 94.8 ± 04% entrapment-efficiency, 62.3 ± 29% loading, and 86.63% release after 6 hrs. MTT assay showed, Ru-SLNs have 15.37 times more effectiveness against melanoma cells, while fluorescence microscopy confirmed the cellular uptake over time. Gel based Ru-SLNs, have reduction in flux across skin, indicating a sustained release of rutin and higher retention within the deeper epidermis layer. Finally, Ru-SLNs based gel exhibited promising potential and effectively targeting to skin’s epidermal layer for melanoma cells. [ABSTRACT FROM AUTHOR]

Study was to develop a nanostructured-lipid-careers (NLCs) of paliperidone (PLP) for nose-to-brain targeting. NLCs was prepared by sonication, high-shear homogenisation method, and characterised their mean diameter, PDI, zeta-potential, morphology (by SEM, TEM and AFM), entrapment efficiency, drug loading, in vitro release, interaction study (by FTIR), and stability. Further, ex vivo permeation and ciliotoxicity performed in sheep nasal mucosa, and in vivo biodistribution/pharmacokinetic was performed in rats for schizophernia. Developed NLCs showed spherical and clearly 3-dimentinal structure with 129 ± 2.7 nm mean diameter, 0.304 ± 0.003 PDI, −7.61 ± 0.56 mV zeta-potential, 58.16 ± 0.17% entrapment efficiency, 65.8 ± 2% drug loading and 74.32 ± 0.003% release in 12 h, followed by Higuchi model. Ex vivo study showed NLCs have three times higher permeation, compare to pure drug (around 71.50.32% in 6 h) and 3.98 g/cm2/h steady sate flux. The blood/brain ratio given by intranasally have higher compare to IV route, and 94.53 ± 21.45% drug targeting efficiency in brain. In conclusion, NLCs have easily crossed BBB, higher drug delivery and effective for schizophrenia in given by intranasal. [ABSTRACT FROM AUTHOR]

AbstractPrimaquine (PQ) is a widely used antimalarial drug, but its high dosage requirements can lead to significant tissue damage and adverse gastrointestinal and hematological effects. Recent studies have shown that nanoformulations can enhance the bioavailability of pharmaceuticals, thereby increasing efficacy, reducing dosing frequency, and minimizing toxicity. In this study, PQ-loaded PLGA nanoparticles (PQ-NPs) were prepared using a modified double emulsion solvent evaporation technique (w/o/w). The PQ-NPs exhibited a mean particle size of 228 ± 2.6 nm, a zeta potential of +27.4 mV, and an encapsulation efficiency of 81.3 ± 3.5%. Scanning electron microscopy (SEM) confirmed their spherical morphology, and the in vitro release profile demonstrated continuous drug release over 72 h. Differential scanning calorimetry (DSC) thermograms indicated that the drug was present in the nanoparticles, with improved physical stability. Fourier-transform infrared spectroscopy (FTIR) analysis showed no interactions between the various substances in the NPs. In vivo studies in Swiss albino mice infected with Plasmodium berghei revealed that the nanoformulated PQ was 20% more effective than the standard oral dose. Biodistribution studies indicated that 80% of the NPs accumulated in the liver, highlighting their potential for targeted drug delivery. This research demonstrates the successful development of a nanomedicine delivery system for antimalarial drugs, offering a promising strategy to enhance treatment efficacy while reducing adverse effects. [ABSTRACT FROM AUTHOR]

The present work is focus on development of anti-psoriasis activity of Karanjin (isolated from Pongamia pinnata seed oil) loaded liposome based lotion for enhancement of skin permeation and retention. Karanjin was isolated using liquid-liquid extraction method and characterised by HPLC analysis and partition coefficient. Further, isolated Karanjin was loaded into liposomes using thin-film hydration technique and optimised by Box-Behnken design. Selected optimised batch was characterised their mean diameter, PDI, zeta potential, and entrapment efficiency, morphology (by TEM), FTIR and ex-vivo skin retention. Additionally, Karanjin loaded liposomes were formulated into lotion and characterise their rheological, spreadability, texture, ex-vivo skin permeation & retention, stability and anti-psoriatic activity in mouse tail model. The yield of Karanjin from seed oil was 0.1% w/v and have lipophilic nature. The optimised liposomal formulation showed 195 ± 1.8 nm mean diameter, 0.271 ± 0.02 PDI, −27.0 ± 2.1 mV zeta potential and 61.97 ± 2.5% EE. TEM image revel the spherical shap of liposome surrounded by single phospholipid bilayer and no interection between drug and excipients. Further, lotion was prepared by 0.1% w/v carbopol and found to 615 mPa.sec viscosity, good thixotropic behaviour, spreadability and texture. There was 22.44% increase in drug permeation for Karanjin loaded liposomal lotion compared to pure Karanjin lotion, confirm by ex-vivo permeation and retention. While, in-vivo study revel the liposomal lotion of Karanjin was found to have 16.09% higher drug activity then 5% w/w conventional Karanjin lotion. Karanjin loaded liposomal lotion have an effective anti-psoriatic agent and showed better skin permeation and retention than the conventional Karanjin lotion. [ABSTRACT FROM AUTHOR]

Several therapeutic agents are used for controlling brain diseases, but they are not successfully reaching target sites due to the complex nature of the brain. Nasal administration as an alternate administration route has been proposed for brain targeting. To solve the above limitation linked to brain targeting through the transmission of nasal products, encourage the production of novel drug delivery by the combination of nanotechnology. The present review focuses on the latest understanding of pathways underlying central nervous system intranasal transmission. Novel Drug delivery systems as important methods for targeting the brain without toxicity in the nasal mucosa and central nervous system, they have acquired the capacity of CNS. [ABSTRACT FROM AUTHOR]

Aim: The goal of this study is to optimisation and evaluation of dopamine-loaded NLC (NLCDOPA) for achieve dopamine concentrations into brain for treatment of Parkinson's disease which causes progressive neuronal death. Method: NLC-DOPA prepared by homogenisation method using solid lipids (Cholesterol and Soya lecithin), liquid lipid (Oleic acid) and surfactant (Poloxamer-188) as major excipients, optimised by central composite design using design expert-13 software. The optimised formulations were characterised by particle size, zeta potential, entrapment efficiency, SEM, TEM, FTIR, DSC, XRD, stability study and in-vitro drug release. The histopathology of rat brain tissues and goat nasal tissues were performed. The ex-vivo (permeability and nasal ciliotoxicity study) and in vivo pharmacodynamics study were also accomplished to determine its efficacy and potency of NLC. Result: The NLC-DOPA formulations were optimised in particle size and (EE)% with range from 85.53 ± 0.703 to 106.11 ± 0.822 nm and 82.17 ± 0.794 to 95.45 ± 0.891%, respectively. The optimised formulation F11 showing best goodness-fitted model kinetic, followed by Korsmeyer- Peppas equation and zero order kinetic. The SEM and TEM confirmed the spherical and smooth morphology of formulation. FTIR and DSC spectra were given compatibility of compound and XRD diffractograms confirmed the amorphous nature. An ex-vivo study was showed the high permeability coefficient (6.67*1 0-4 cm/min, which is twice, compare to pure drug) and there was no damage in nasal mucosa, confirmed by the ciliotoxicity study. In-vivo study was shown significant effects of optimised NLC-DOPA on locomotor activity, force-swimming test and neurochemical assessment using rotenone induced Parkinson's model on Albino Wistar rats. Conclusion: NLC-DOPA was prepared and optimised successfully with increased bioavailability of drug from the NLC into brain with reduce toxicity in effective treatment of Parkinson's disease. [ABSTRACT FROM AUTHOR]

Berberine is an anticancer medication that generates side effects due to its hydrophobicity and low cellular promiscuity as well as high dose requirement. Thus, have to prepare PEGylated dendrimer conjugates which increases the targeting and release of chemotherapeutic drugs at the tumor site although falling the adverse side effects. The circulation time of drug is enhanced by PEGylation. It is the covalent attachment of PEG to therapeutic protein or any molecule. PEGylated berberine dendrimer was prepared by biotinylation cross linking method and characterized by particle size, zeta potential, entrapment efficiency, in vitro release and stability study. The Structure validation of berberine before and after grafting was confirmed by FTIR and NMR spectroscopy. Further prepared PEGylated complex were proceeded for the cellular uptake study in AMJ-13, and BT-20 cells line by fluorescent microscopy study and MTT assay cytotoxicity study in MCF-7 cell line. The prepared PEGylated formulation showed nanometric size, desired zeta potential, and 69.56 ± 23% entrapment efficiency. The prepared PEGylated particle showed 70.23% release at 72 h with good stability at 90 days. The cellular uptake of formulation was highly appreciable which is clearly observed in AMJ-13 and BT-20 cells line. In comparison to pure drug, developed formulation has 10.8 M high efficiency for breast cancer cell line. PEGylation is easy and reasonable way, as it requires lesser time and is proved to be superior technique for treatment of cancer. [ABSTRACT FROM AUTHOR]

The study was to extend systemic circulation and biological half-life (t1/2) of trans-resveratrol (RSV) using solid lipid nanoparticles (RSV-SLN) to improve its anti-cancer potential. RSV-SLN was prepared by solvent emulsification evaporation technique and proceeded for evaluation like particle size, PDI, zeta potential, in vitro release, in vitro cytotoxicity, cellular internalisation, haemolysis and erythrocyte membrane integrity, platelet aggregation and pharmacokinetic studies in rats. Moreover, cancer cells accumulation of RSV-SLN also needs to be evaluated for proving their targeting ability. Prepared SLN showed 126.85 ± 12.09 nm particle size, −24.23 ± 3.27 mV Zeta potential and 74.67 ± 4.76%. release at 48 h and haemocompatible. The cellular internalisation image showed the SLN reach in a cytoplasm and nucleus of PC3 prostate cells. RSV-SLN exhibited high t1/2 (8.22 ± 1.36 h) and 7.19 ± 0.69 h MRT (Mean residence time) and lower clearance i.e. 286.42 ± 13.64 mL/min/kg. The bio-distribution of RSV-SLN was found to be extremely high in prostate cells and accumulate 7.56 times greater than that of RSV solution. The developed RSV-SLN can be applied as potential carrier for delivery of drug of chemotherapeutics at an extend systemic circulation and targeting efficiency at tumour site. [ABSTRACT FROM AUTHOR]

The research focussed on development and evaluation of ethosome as an effective delivery of antigen that eliminates need for frequent dose of antigen while improving patient compliance for Hepatitis B. Prepared a single dose HBsAg ethosomal vaccine using a cold method and applied a central composite design optimisation using particles size, zeta potential and entrapment efficiency as dependent variables. Further, selected batch was assessed for their morphology, in vitro release, interaction, haemocompatibility, histological (ex vivo skin permeation) and stability studies. Further, proceeded for in-vivo study, administered in BALB/c mice via nasal route to check the immunological activity and compared with single and multiple doses of ethosome to booster doses of alum-HBsAg vaccine. Immunological marker like immunoglobulin (IgG and IgA) and cytokines (interleukin-2 and interferon-Y) were measured by ELISA techniques. The prepared ethosome showed minimum particle size (93.98 ± 4.6), 15.0 ± 2.83 mV zeta potential, with maximum entrapment efficiency (66.25 ± 8.6%). Physicochemical characterisation reveal the sustained release, haemocampatibile, and stable nature of ethosome. Further, ex-vivo skin permeation showed safely administration of drug by nasal route without toxicity. The in vivo study, found the higher immunological response observed in BALB/c mice, compare to alum-HBsAg vaccine. The single dose of ethosome showed sufficient effective and measurable immunoglobulin and cytokines levels. A single dose of ethosome is sufficient for the complete immunological response not require booster administration. The potency of ethosomes have to produce a protective immune response, as well as their ability to explore and target the immunological environment through nasal route. [ABSTRACT FROM AUTHOR]

The current study focussed on the development and evaluation of aqueous core nanocapsules (ACNs) as an effective carrier to deliver an optimal synergistic combination of a highly water-soluble Vinorelbine bitartrate (VRL) and a poorly water-soluble Resveratrol (RES) for treatment of breast cancer. Various molar ratios of VRL to RES were screened against MCF-7 cell lines to determine the synergistic effects using the Chou-Talalay method. The synergistic ratio of therapeutic agents was then incorporated into aqueous core nanocapsules utilising a double emulsion solvent evaporation technique to yield dual drug-loaded nanocapsules (dd-ACNs). The dd-ACNs were optimised using Box-Behnken design and characterised for physicochemical parameters such as particle size, zeta potential, polydispersity index, total drug content and encapsulation efficiency, surface morphology, drug excipient compatibility by FTIR and DSC, release kinetics, toxicity studies and anticancer efficacy (in-vitro and in-vivo). Results demonstrated that the combination exhibited maximum synergy when higher doses of VRL were combined with smaller doses of RES (1:1, 5:1, and 10:1). The dual drug-loaded ACNs were found to be stable and depicted a core-shell structure, narrow size range (150.2 ± 3.2 nm) with enhanced encapsulation (80% for VRL and 99% for RES). Moreover, the dd-ACNs were 5 times more efficacious in-vitro than a combination of free drugs, while reducing systemic toxicity. Also, pre-clinical evaluation of dd-ACNs also depicted a drastic reduction of tumour volume as compared tp pristine VRL and a physical combination of drugs. The developed dd-ACNs can be applied as a potential carrier for delivery of a combination of chemotherapeutics at a synergistic ratio at the tumour site. [ABSTRACT FROM AUTHOR]

This work studies the development and evaluation of Gymnema sylvestre (GYM) extract loaded sustained release polymeric nanoparticles (PNPs) for enhanced bioavailability and reduced nephrotoxicity. The current therapy is associated with the drawbacks of addiction and repeated administration. The sustained release PNPs were developed and evaluated for toxicity. PNPs of GYM were prepared by double emulsion solvent evaporation technique utilising Taguchi model and evaluated for physicochemical properties (particle size, zeta potential, entrapment efficiency), in vitro drug release, compatibility, and stability. Further, the bioavailability and in vivo nephrotoxicity studies in diabetic rat model were also carried out. The developed optimised nanoparticles were 205.7 ± 1.20 nm in size, −40.68 mV zeta potential, compatible, and stable in nature with improved entrapment efficiency (67.1 ± 0.2%) and sustained release. Moreover, nanoparticles were found to lower the blood glucose level in single as well as multiple doses. Results of in vivo study indicated that GYM-NPs increased the phosphorylase activity and thus enhanced insulin secretion. Furthermore, the nanoparticles were free from toxicity, which was confirmed by the estimation of kidney biomarker. The nanoparticles increased the bioavailability of GYM extract and have a great potential for the treatment of diabetes in reduced dose, and so these can be potential candidates for treating diabetes. [ABSTRACT FROM AUTHOR]

Migraine is a frequent neurological condition characterized by throbbing headaches, nausea, photophobia, and phonophobia, among other symptoms. Sumatriptan belongs to a BCS class III, which exhibits poor oral bioavailability and several side-effects. The objective of the present study was to develop solid lipid nanoparticles (SLNPs) of sumatriptan succinate for brain targeting by nasal route. Solvent injection method was used to increase the entrapment efficiency of hydrophilic drug. Thus, formulation was optimized by central composite design with minimum particle size, optimized zeta potential, and maximum entrapment efficiency, which was found to be 133.4 nm, −17.7 mV, and 75.5%, respectively. Optimized batch was further evaluated for surface morphology, Fourier-transform infrared spectroscopy, in vitro release, permeation across nasal mucosa, and histopathology. It was seen that most of the particles were spherical in shape as confirmed by scanning electron microscopy and transmission electron microscopy. The release of drug through the lipid showed initial burst release followed by sustained release up to 12 h. The ex vivo diffusion study using goat nasal mucosa at pH 6.8 revealed that SLNPs permeation across nasal mucosa was quick, which was sufficient for brain targeting. Histopathology studies further revealed integrity of nasal mucosa after treatment with SLNPs. The investigation indicated that hydrophilic drug, sumatriptan succinate can be successfully entrapped in SLNPs to target brain via nasal delivery, and thus it could be an effective approach for nose-to-brain delivery. [ABSTRACT FROM AUTHOR]

PEGylation is the covalent addition of PEG to one more molecule. PEGylation can improve the maintenance time of the therapeutics similar to proteins, liposomes, and nanoparticle through shielding them beside different debasing mechanisms dynamic in a body that improve beneficial properties. This skill is used to get better half-life and other pharmaceutical properties of a protein, peptide, or non-peptide molecule. Polyethylene glycol is harmless, non-immunogenic, non-antigenic, and extremely soluble in water and FDA accepted polymer. It shows a significant role in drug delivery. A variety of PEG-based formulations are available in the market. This paper represents the benefits of PEGylation over non-PEGylated products. Now a day, PEGylation plays an important role in the drug delivery system. PEGylation increases the therapeutic potential of drugs. [ABSTRACT FROM AUTHOR]

Chronic Hepatitis B Virus (HBV) infections are severe with weak antiviral immune responses. The lack of an appropriate small animal model for chronic hepatitis, a major hurdle for studying the immunotolerance and immunopathogenesis induced by hepatitis B viral (HBV) infection. In this study, for enhancing the antibody production efficiency the prepared polymeric HBsAg-loaded nanoparticles (nanovaccine) will be tested in immune-deficit mice, which suffer from chronic Hepatitis B virus. Vaccination of Balb/c mice by this prepared nanoparticles that were engrafted with peripheral blood mononuclear cells (PBMCs), which was already lethally irradiated and transplanted by the bone marrow of NOD (knockout mice) mice. In the present study, after the vaccination detected the high frequencies of immunoglobulin G (IgG)-secreting B cells and mitogen-responsive interferon-Y (IFN-Y) secreting T cells in serum, determined by specific ELISA technique. During the entire observation period, unvaccinated animals showed lower concentration of specific IgG secreting B cells and IFN-Y secreting T cells found in comparison to vaccinated mice group. Chronic HBV carrier PBMCs transplanted into the chimera failed to produce antigen and increased the antibodies production due to vaccination. Furthermore, another advantage was that the viral gene expression and viral DNA replication was no longer observed in vaccinated group. This prepared nanovaccine formulations is better for the cure of Hepatitis B viral infection carrier. Therefore, specific memory responses were elicited by vaccination with Hepatitis B virus surface (HBsAg) antigen of chimeric mice transplanted with PBMCs derived from HBV donors. [ABSTRACT FROM AUTHOR]