Mechanistic insights of desmopressin loaded elastic liposomes for transdermal delivery: HSPiP predictive parameters and instrumental based evidences.

Desmopressin acetate (DA) is a first-line option for the treatment of hemophilia A, von Willebrand's disease, nocturnal enuresis, central diabetes insipidus, and various traumatic injuries. We extended previously reported desmopressin-loaded elastic liposomes (ODEL1) to investigate mechanistic insights into ODEL1 mediated augmented permeation across rat skin. HSPiP software and instrumental techniques such as differential scanning calorimeter (DSC), Fourier Transform infrared (FTIR), scanning electron microscopy (SEM), and fluorescent microscopy provided better understandings of permeation behavior.

A Green Approach: Optimization of the UPLC Method Using DoE Software for Concurrent Quantification of Pioglitazone and Dapagliflozin in a SNEDDS Formulation for the Treatment of Diabetes.

Clinical trials revealed that pioglitazone (PGZ) and dapagliflozin (DGZ) not only maintain normal blood glucose levels but also reduce complications of diabetes mellitus. To meet the demand for simultaneous measurement of these drugs in fixed combinations, an optimized and green UPLC method is required. The present study utilized Design of Experiments (DoE) software to optimize analytical parameters for simultaneous drug analysis.

Optimization of Glibenclamide Loaded Thermoresponsive SNEDDS Using Design of Experiment Approach: Paving the Way to Enhance Pharmaceutical Applicability.

Thermoresponsive self-nanoemulsifying drug delivery systems (T-SNEDDS) offer a promising solution to the limitations of conventional SNEDDS formulations. Liquid SNEDDS are expected to enhance drug solubility; however, they are susceptible to leakage during storage. Even though solid SNEDDS offers a solution to this storage instability, they introduce new challenges, namely increased total dosage and potential for drug trapping within the formulation.

HSPiP and QbD oriented optimized stearylamine-elastic liposomes for topical delivery of ketoconazole to treat deep seated fungal infections: In vitro and ex vivo evaluations.

The study explored stearylamine containing cationic elastic liposomes to improve topical delivery and efficacy of ketoconazole (KETO) to treat deeply seated fungal infections. Stearylamine was used for dual functionalities (electrostatic interaction and flexibility in lipid bilayer). Hansen solubility program (HSPiP) estimated Hansen solubility parameters (HSP) based on the SMILE file and structural properties followed by experimental solubility study to validate the predicted values.

Solubility and thermodynamic analysis of aceclofenac in different {Carbitol + water} mixtures at various temperatures.

The solubility and thermodynamic properties of the anti-inflammatory drug aceclofenace (ACF) have been assessed in a range of {2-(2-ethoxyethoxy)ethanol (Carbitol) + water} combinations at temperatures ranging from 298.2 K to 318.2 K and atmospheric pressure of 101.

HSPiP, Computational, and Thermodynamic Model-Based Optimized Solvents for Subcutaneous Delivery of Tolterodine Tartrate and GastroPlus‑Based In Vivo Prediction in Humans: Part II.

In part I, we reported Hansen solubility parameters (HSP, HSPiP program), experimental solubility at varied temperatures for TOTA delivery. Here, we studied dose volume selection, stability, pH, osmolality, dispersion, clarity, and viscosity of the explored combinations (I-VI). Ex vivo permeation and deposition studies were performed to observe relative diffusion rate from the injected site in rat skin.

Potentially active aspirin derivative to release nitric oxide: , and approaches.

The series of newer salicylate derivatives incorporating nitroxy functionality were synthesized and evaluated for their potential effect in gastrointestinal (GI) related toxicity produced by aspirin. The synthesized compounds (5a-j) were subjected to %NO (nitric oxide) release study, anti-inflammatory potential, % inhibition of carrageenan-induced paw edema and the obtained results were validated by studies including molecular docking, MD simulations and ADME (absorption, distribution, metabolism, and elimination) calculations. Compounds 5a (20.

HSPiP, Computational Modeling, and QbD-Assisted Optimized Method Validation of 5-Fluorouracil for Transdermal Products.

This study addressed the simplest and most efficient HPLC (high-performance liquid chromatography) method for the estimation of 5-fluorouracil (5-FU) from rat blood plasma by implementing the Hansen solubility parameters (HSP), computation prediction program, and QbD (quality by design) tool. The mobile phase selection was based on the HSP predictions and experimental data. The Taguchi model identified seven variables (preoptimization) to screen two factors (mobile phase ratio as A and column temperature as B) at three levels as input parameters in "CCD (central composite design)" optimization (retention time as and peak area as ).

HSPiP and QbD Program-Based Analytical Method Development and Validation to Quantify Ketoconazole in Dermatokinetic Study.

Ketoconazole (KTZ) is the most potential azole anti-mycotic drug. The quantification of KTZ from various layers of the skin after topical application of lipidic nanocarriers is critical. We addressed a sensitive, specific, simple, rapid, reproducible, and economic analytical method to quantify KTZ from the treated skin homogenate using the Hansen solubility parameter (HSP, HSPiP software)-based modeling and experimental design.

Hansen Solubility Parameters and QbD-Oriented HPLC Method Development and Validation for Dermatokinetic Study of a Miconazole-Loaded Cationic Nanoemulsion in Rat Model.

Miconazole (MCZ) is a potential antifungal drug to treat skin infections caused by , (athlete's foot fungal infection), (jock itching in the groin and buttocks), and (red scaly rash on the skin). The current study focused on Hansen parameter-based solvent selection (HSPiP software) and method development optimization using an experimental design tool for sensitive, accurate, reproducible, economic, rapid, robust, and precise methodology to quantify MCZ in rat plasma. Moreover, a Taguchi design was used for screening two independent factors (flow rate and ACN content).

Formulation of Silymarin-β Cyclodextrin-TPGS Inclusion Complex: Physicochemical Characterization, Molecular Docking, and Cell Viability Assessment against Breast Cancer Cell Lines.

Silymarin (SIL) is a poorly water-soluble flavonoid reported for different pharmacological properties. Its therapeutic applications are limited due to poor water solubility. In this study, the solubility of silymarin has been enhanced by preparing freeze-dried binary and ternary complexes using beta cyclodextrin (βCD) and d-α-tocopherol polyethylene glycol 1000 succinate (TPGS).

Mechanistic of Vesicular Ethosomes and Elastic Liposomes on Permeation Profiles of Acyclovir across Artificial Membrane, Human Cultured EpiDerm, and Rat Skin: In Vitro-Ex Vivo Study.

Acyclovir (ACV) controls cutaneous herpes, genital herpes, herpes keratitis, varicella zoster, and chickenpox. From previously reported ACV formulations, we continued to explore the permeation behavior of the optimized ACV loaded optimized ethosome (ETHO2R) and elastic liposome (ELP3R) and their respective carbopol gels across artificial membrane, cultured human EpiDerm, and rat skin. Transepidermal water loss (TEWL), scanning electron microscopy (SEM), confocal laser scanning microscopy (CLSM), and atomic force microscopy (AFM) were used to investigate the mechanistic perspective of permeation behavior.

Formulation of multicomponent inclusion complex of cyclodextrin-amino acid with Chrysin: Physicochemical characterization, cell viability and apoptosis assessment in human primary glioblastoma cell line.

Chrysin (CR) is a water-insoluble drug reported for different therapeutic effects. The microwave irradiation method was used in this study to create a multicomponent inclusion complex (CR-MC) containing CR (drug) and carrier hydroxyl propyl beta cyclodextrin (HP β CD) and L-arginine (LA). The prepared inclusion complex (CR-MC) was evaluated for dissolution study and results were compared with chrysin physical mixture (CR-PM).

GastroPlus- and HSPiP-Oriented Predictive Parameters as the Basis of Valproic Acid-Loaded Mucoadhesive Cationic Nanoemulsion Gel for Improved Nose-to-Brain Delivery to Control Convulsion in Humans.

Oral and parenteral delivery routes of valproic acid (VA) are associated with serious adverse effects, high hepatic metabolism, high clearance, and low bioavailability in the brain. A GastroPlus program was used to predict in vivo performance of immediate (IR) and sustained release (SR) products in humans. HSPiP software 5.

Biogenic nanoparticles from waste fruit peels: Synthesis, applications, challenges and future perspectives.

Nanotechnology is a continually growing field with a wide range of applications from food science to biotechnology and nanobiotechnology. As the current world is grappling with non-biodegradable waste, considered more challenging and expensive to dispose of than biodegradable waste, new technologies are needed today more than ever. Modern technologies, especially nanotechnology, can transform biodegradable waste into products for human use.

Formulation of Piperine-Loaded Nanoemulsion: In Vitro Characterization, Ex Vivo Evaluation, and Cell Viability Assessment.

Piperine is an alkaloid, but its therapeutic efficacy is limited due to poor aqueous solubility. In this study, piperine nanoemulsions were prepared using oleic acid (oil), Cremophore EL (surfactant), and Tween 80 (co-surfactant) using the high-energy ultrasonication approach. The optimal nanoemulsion (N2) was further evaluated using transmission electron microscopy, release, permeation, antibacterial, and cell viability studies based on minimal droplet size and maximum encapsulation efficiency.

HPV pathogenesis, various types of vaccines, safety concern, prophylactic and therapeutic applications to control cervical cancer, and future perspective.

Over 98% of cervical cancers (CC) are caused by regular infections with "high risk" genotype of the human papilloma virus (HPV). However, this is not always the causative factor. Therefore, production of HPV vaccinations represents a significant chance to minimize the risk of CC.

Optimized Green Nanoemulsions to Remove Pharmaceutical Enoxacin from Contaminated Bulk Aqueous Solution.

We attempted to develop green nanoemulsions (ENE1-ENE5) using capryol-C90 (C90), lecithin, Tween 80, and -methyl-2-pyrrolidone (NMP). HSPiP software and experimentally obtained data were used to explore excipients. ENE1-ENE5 nanoemulsions were prepared and evaluated for in vitro characterization parameters.

Identification of Potential Antitubulin Agents with Anticancer Assets from a Series of Imidazo[1,2-]quinoxaline Derivatives: In Silico and In Vitro Approaches.

Computer-aided drug design is a powerful and promising tool for drug design and development, with a reduced cost and time. In the current study, we rationally selected a library of 34 fused imidazo[1,2-]quinoxaline derivatives and performed virtual screening, molecular docking, and molecular mechanics for a lead identification against tubulin as an anticancer molecule. The computational analysis and pharmacophoric features were represented as ; this was a potential lead against tubulin, with a maximized affinity and binding score at the colchicine-binding site of tubulin.

Strategic nanocarriers to control neurodegenerative disorders: Concept, challenges, and future perspective.

Various neurodegenerative diseases (parkinson, huntington, alzheimer, and amyotrophic lateral sclerosis) are becoming serious global health challenges. Despite various treatment options, successful delivery and effective outcomes have been challenged with several physiological-anatomical barriers, formulation related issues, post-administration hurdles, regulatory constraints, physical hurdles, environmental issues, and safety concern. In the present review, we addressed a brief understanding of pathological and normal condition of blood brain barrier (BBB), rational for brain delivery using nanocarriers, major challenges, advantages of nanomedicine, critical aspects of nanomedicine to translate from bed to clinics, and strategic approaches for improved delivery across BBB.

Mechanistic Insights into Luteolin-Loaded Elastic Liposomes for Transdermal Delivery: HSPiP Predictive Parameters and Instrument-Based Evidence.

We evaluated mechanistic insights into luteolin (LUT)-loaded elastic liposomes (OLEL1) permeated across rat skin. HSPiP software-based parameters, thermal analysis, infrared analysis, and morphological evaluations were employed to understand mechanistic observations of drug permeation and deposition. HSPiP provided HSP values (δ, δ, and δ) of OLEL1 (based on composition), LUT, excipients, and rat skin (literature value and by-default value).

Green Nanoemulsion Water/Ethanol/Transcutol/LabM-Based Treatment of Pharmaceutical Antibiotic Erythromycin-Contaminated Aqueous Bulk Solution.

Contaminated wastewater released from hospital, domestic, and industrial sources is a major challenge to aquatic animals and human health. In this study, we addressed removal of erythromycin (ERN) from contaminated water employing water/ethanol/Transcutol/Labrafil M 1944 CS (LabM) green nanoemulsions as a nanocarrier system. ERN is a major antibiotic contaminant harming aquatic and human lives.

Formulation of Multicomponent Chrysin-Hydroxy Propyl β Cyclodextrin-Poloxamer Inclusion Complex Using Spray Dry Method: Physicochemical Characterization to Cell Viability Assessment.

The work aimed to enhance chrysin (CHR) water solubility, dissolution, and in vitro antibacterial as well as cell viability. Chrysin binary, as well as ternary inclusion complex, were prepared using the spray drying method. The influence of an auxiliary component (poloxamer; PLX) was also assessed after being incorporated into the chrysin HP βCD complex (CHR-BC) and formed as a chrysin ternary complex (CHR-TC).

Hydroethanolic Extract of L. (Stinging Nettle) Leaves as Disaccharidase Inhibitor and Glucose Transport in Caco-2 Hinderer.

Herbal treatment for diabetes mellitus is widely used. The pharmacological activity is thought to be due to the phenolic compounds found in the plant leaves. The present study aims to investigate the phytochemical composition of (UD) hydroethanolic extract and to screen its antidiabetic activity by disaccharidase hindering and glucose transport in Caco-2 cells.