Neusilin US2 Research Articles

Self-microemulsifying drug delivery system (SMEDDS) for oral delivery of zafirlukast: Design, formulation, and pharmacokinetic evaluation

The current research aimed to develop a self-microemulsifying drug delivery system (SMEDDS) of zafirlukast to enhance its oral bioavailability by increasing its solubility and overcoming the negative food effect. For the formulation of SMEDDS, the solubility of zafirlukast was determined in different oils, surfactants, and cosurfactants. Based on this study's results, pseudo-ternary phase diagrams were plotted to select the efficient self-emulsification region. Eudragit EPO was employed as a precipitation inhibitor to avoid the supersaturation of zafirlukast in the SMEDDS system. The formulated system was evaluated for transparency, cloud point, optical birefringence, and globule size analysis using techniques like DLS, SANS and TEM. The SMEDDS preconcentrate was solidified by adsorbing it on Neusilin US2 and further formulated as a tablet. It was then evaluated for in vitro drug release against the marketed tablet. The optimized composition of zafirlukast SMEDDS and suspension of the plain drug were evaluated for a pharmacokinetic profile in rats for both fed and fasted conditions. The SMEDDS yielded microemulsion found transparent and homogeneous with globule size less than 50 nm by DLS, SANS and TEM techniques. On dilution with water, the microemulsion was found robust without any phase separation even after 24 h of storage. The tablet form of SMEDDS was stable and passed all the IPQC tests for a tablet. The optimized SMEDDS tablet form exhibited a superior in vitro dissolution profile than a marketed tablet. The pharmacokinetic study of optimized SMEDDS showed improved value for Cmax and AUC in both fed and fasted conditions compared to the plain drug.

Quality by Design Optimization of Telmisartan-loaded Self-nanoemulsifying Drug Delivery Systems

Aim: This study aimed to develop a QbD-based SNEDDS for Telmisartan to enhance its biopharmaceutical performance. Background: Quality by Design (QbD) was incorporated by selecting the Critical Process Pa-rameters (CPPs) as influential variables upon the desired responses. Using Design of Experiments (DoE) software, oil, and S/CoS were tested for pre-isotropic compatibility and formulation im-provement. A heating-cooling cycle and phase separation were used to determine the formula-tions' dispersibility, self-emulsifying time, mean globule size, and stability. Objective: Using Design of Experiments (DoE) software, oil (Capmul MCM C-10) and surfactant (Labrasol)/co-surfactant (Tween-20, and PEG-600) (S/CoS) ratios were optimized for pre-isotropic compatibility and formulation improvement. Methods: Aerosil-200, Sylysia-350, 550, and 730 were used as porous carriers, and Neusilin US2 as an adsorbing agent resulted in free-flowing granules of self-nano emulsifying drug delivery systems. The SNEDDS was further formulated into tablets using a direct compression technique with enhanced disintegration properties. Results: The prepared SNEDDS tablets exhibited a 71% increase in drug dissolution as compared to the pure drug and marketed formulation after the in vitro dissolution studies. Conclusion: This QbD approach offers a promising strategy for developing SNEDDS formula-tions for poorly soluble drugs like Telmisartan.

Solidification of deep eutectic solvent containing fimasartan through wet impregnation and exploration of flow attributes by modified SeDeM-SLA expert system

The solidification of deep eutectic solvent (DES) through wet impregnation techniques on inert solid carriers is an interesting approach that offers better processing attributes and excellent stability. Herein, DES of Fimasartan (FS) was developed to improve its solubility and bioavailability. The selected DES-FS was solidified by wet impregnation method employing Nesulin US2 and Aerosil 200. The SeDeM-SLA (solid–liquid adsorption) system was employed to investigate flow attributes of solidified DES-FS. Further, the selected solidified DES-FS (A) was characterized by Fourier transforms infrared spectroscopy (FTIR), Powder X-ray diffraction (PXRD), Differential scanning calorimetry (DSC), Scanning electron microscopy (SEM). The DES comprising Choline Chloride (ChCl): Glycerol (Gly) (1:3) revealed maximum drug solubility (35.6 ± 2.2 mg/mL) and thus opted for solidification. Solidification through wet impregnation was employed using 1:0.5 ratios (DES-FS to carriers). The Index of Good Flow (IGF) value was calculated from the SeDeM-SLA expert system, which indicates the better flow characteristics of solidified DES-FS, particularly with Neusilin US2 [SDES-FS (A)]. The solid-state evaluation data of SDS-FS (A) suggested a transition of FS to an amorphous form, resulting in an increment in solubility and dissolution. A similar trend was reported in the in vivo pharmacokinetic study, which indicated a 2.9 folds increment in the oral bioavailability of FS. Furthermore, excellent stability, i.e., a shelf life of 28.44 months, reported by SDES-FS (A) in accelerated stability studies, suggests better formulation perspectives. In a nutshell, the present study evokes the potentiality of performing solidification through wet impregnation and successful implementation of the SeDeM-SLA expert model, which could find wide applications in pharmaceutical science.

Formulation, Optimization and Evaluation of Ticagrelor Liquisolid Tablets for Enhanced Solubility

Purpose The study aims to use liquisolid compacts technology as a novel carrier to enhance Ticagrelor's solubility and release profile. Method: Formulation of liquisolid tablets was developed using the Design of Experiment (DOE) approach where the drug Ticagrelor was dispersed in PEG-600 and incorporated into carrier material (Neusilin US2) in the mortar, the liquid drug was permitted to absorb in the second stage. Aerosil-200 was used as a coating material, and Magnesium stearate and Sodium starch Glycolate were used as Lubricant and Disintegrating Agent respectively. The formulations were optimized and the carrier-to-coating ratio and mixing Aerosil-200 with Neusilin US2 effect on drug release from the formulation was investigated. The prepared liquisolid compacts were subjected to micrometric characterization, post-compression parameters, Fourier Transform Infrared Spectroscopy (FTIR), and Differential Scanning Calorimetry (DSC). Result: The cumulative drug release of all formulations in dissolution media varies from 82% to 96% and Formulation F9 showed a maximum cumulative drug release of about 96%. The drug contents of all formulations ranged from 91.06% to 99.01%. Disintegration time for all 1-9 formulations, clearly, all compositions disintegrate in less than 10 minutes. The cumulative drug release of all formulations varies from 82% to 96% Formulation F9 showed a maximum cumulative drug release of about 96% and the conventional tablet showed a cumulative drug release of about 80 %. The optimized liquisolid formulation F8 outperformed the other batches in terms of flow and compressibility across all formulations. Conclusion: Therefore, as per the results, it can be inferred that Ticagrelor, when formulated by a liquisolid approach, produce ameliorated dissolution and stability profile.

Comparison of the liquisolid technique and co-milling for loading of a poorly soluble drug in inorganic porous excipients

Drug loading into mesoporous carriers may help to improve the dissolution of poorly aqueous-soluble drugs. However, both preparation method and carrier properties influence loading efficiency and drug release. Accordingly, this study aimed to compare two preparation methods: formulation into liquisolid systems (LSS) and co-milling for their efficiency in loading the poorly soluble model drug cyclosporine A (CyA) into mesoporous magnesium aluminometasilicate Neusilin® US2 (NEU) or functionalized calcium carbonate (FCC). Scanning electron microscopy was used to visualize the morphology of the samples and evaluate the changes that occurred during the drug loading process. The solid-state characteristics and physical stability of the formulations, prepared at different drug concentrations, were determined using X-ray powder diffraction. In vitro release of the drug was evaluated in biorelevant media simulating intestinal fluid. The obtained results revealed improved drug release profiles of the formulations when compared to the milled (amorphous) CyA alone. The dissolution of CyA from LSS was faster in comparison to the co-milled formulations. Higher drug release was achieved from NEU than FCC formulations presumably due to the higher pore volume and larger surface area of NEU.

Hop Flower Supercritical Carbon Dioxide Extracts Coupled with Carriers with Solubilizing Properties-Antioxidant Activity and Neuroprotective Potential.

Lupuli flos shows many biological activities like antioxidant potential, extended by a targeted effect on selected enzymes, the expression of which is characteristic for neurodegenerative changes within the nervous system. Lupuli flos extracts (LFE) were prepared by supercritical carbon dioxide (scCO2) extraction with various pressure and temperature parameters. The antioxidant, chelating activity, and inhibition of acetylcholinesterase (AChE), butyrylcholinesterase (BChE), and tyrosinase by extracts were studied. The extracts containing ethanol were used as references. The most beneficial neuroprotective effects were shown by the extract obtained under 5000 PSI and 50 °C. The neuroprotective effect of active compounds is limited by poor solubility; therefore, carriers with solubilizing properties were used for scCO2 extracts, combined with post-scCO2 ethanol extract. Hydroxypropyl-β-cyclodextrin (HP-β-CD) in combination with magnesium aluminometasilicate (Neusilin US2) in the ratio 1:0.5 improved dissolution profiles to the greatest extent, while the apparent permeability coefficients of these compounds determined using the parallel artificial membrane permeability assay in the gastrointestinal (PAMPA GIT) model were increased the most by only HP-β-CD.

Co-Dispersion Delivery Systems with Solubilizing Carriers Improving the Solubility and Permeability of Cannabinoids (Cannabidiol, Cannabidiolic Acid, and Cannabichromene) from Cannabis sativa (Henola Variety) Inflorescences.

Cannabinoids: cannabidiol (CBD), cannabidiolic acid (CBDA), and cannabichromene (CBC) are lipophilic compounds with limited water solubility, resulting in challenges related to their bioavailability and therapeutic efficacy upon oral administration. To overcome these limitations, we developed co-dispersion cannabinoid delivery systems with the biopolymer polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol (Soluplus) and magnesium aluminometasilicate (Neusilin US2) to improve solubility and permeability. Recognizing the potential therapeutic benefits arising from the entourage effect, we decided to work with an extract instead of isolated cannabinoids. Cannabis sativa inflorescences (Henola variety) with a confirming neuroprotective activity were subjected to dynamic supercritical CO2 (scCO2) extraction and next they were combined with carriers (1:1 mass ratio) to prepare the co-dispersion cannabinoid delivery systems (HiE). In vitro dissolution studies were conducted to evaluate the solubility of CBD, CBDA, and CBC in various media (pH 1.2, 6.8, fasted, and fed state simulated intestinal fluid). The HiE-Soluplus delivery systems consistently demonstrated the highest dissolution rate of cannabinoids. Additionally, HiE-Soluplus exhibited the highest permeability coefficients for cannabinoids in gastrointestinal tract conditions than it was during the permeability studies using model PAMPA GIT. All three cannabinoids exhibited promising blood-brain barrier (BBB) permeability (Papp higher than 4.0 × 10-6 cm/s), suggesting their potential to effectively cross into the central nervous system. The improved solubility and permeability of cannabinoids from the HiE-Soluplus delivery system hold promise for enhancement in their bioavailability.

Screening of the Anti-Neurodegenerative Activity of Caffeic Acid after Introduction into Inorganic Metal Delivery Systems to Increase Its Solubility as the Result of a Mechanosynthetic Approach.

The proven anti-neurodegenerative properties of caffeic acid in vivo are limited due to its poor solubility, which limits bioavailability. Therefore, caffeic acid delivery systems have been developed to improve caffeic acid solubility. Solid dispersions of caffeic acid and magnesium aluminometasilicate (Neusilin US2-Neu) were prepared using the ball milling and freeze-drying techniques. The solid dispersions of caffeic acid:Neu obtained by ball milling in a 1:1 mass ratio turned out to be the most effective. The identity of the studied system in comparison to the physical mixture was confirmed using the X-Ray Powder Diffractionand Fourier-transform infrared spectroscopy techniques. For caffeic acid with improved solubility, screening tests were carried out to assess its anti-neurodegenerative effect. The obtained results on the inhibition of acetylcholinesterase, butyrylcholinesterase, tyrosinase, and antioxidant potential provide evidence for improvement of caffeic acid's anti-neurodegenerative activity. As a result of in silico studies, we estimated which caffeic acid domains were involved in interactions with enzymes showing expression relevant to the neuroprotective activity. Importantly, the confirmed improvement in permeability of the soluble version of caffeic acid through membranes simulating the walls of the gastrointestinal tract and blood-brain barrier further strengthen the credibility of the results of in vivo anti-neurodegenerative screening tests.

Development of Doxazosin mesylate liquisolid system for improved manufacturing processability and bioavailability: in vitro and in vivo evaluation for tailored hypertension treatment approach with modified dissolution rates

In the present research, an attempt was made to optimize the blends of different carriers Neusiln US2, Avicel PH101, and Fujicalin SG by individually blending with each of coating materials Aerosil 200 and Syloid 244 FP that were proposed to contribute to a modified drug dissolution rates of Doxazosin mesylate (DX) through a liquisolid polymer matrix system. The liquisolid formulations were prepared using selected solvent, carriers, and coats by varying drug to polymer ratios. Further formulations were investigated for pre-compression processability by Heckel plot analysis, elastic recovery studies, and post-compression characteristics. In case of carriers, compared to Avicel PH101 highest flowable values (ф) were observed for Neusilin US2 and Fujicalin SG whereas, for coat these values were highest for Aerosil 200 than Sylloid 244 FP. Liquisolid compact with Fujicalin SG and Aerosil 200 exhibited fast release (FR) of 78% in 20 minutes. The liquisolid compact with Neusilin US2 and Syloid 244 FP exhibited prolonged release (PR) of 60% in 240 minutes. DSC and XRD analysis showed loss of DX crystallinity which was confirmed by SEM analysis indicating DX detention within the liquisolid system, in a molecularly dispersed solubilized form. The in vivo studies of DX liquisolid FR formulation exhibited 1.89 fold increase in the oral bioavailability which was 1.69 fold for DX PR formulation compared to pure DX which demonstrated a promising tailored hypertension treatment approach.

Dolutegravir Loaded Solid Self-Micro-Emulsifying Drug Delivery System for Enhanced Solubility and Dissolution

Dolutegravir sodium (DG) is a recently approved antiretroviral drug belonging to BCS class II having poor aqueous solubility and only 16% oral bioavailability. Hence aim of the present work was to develop solid self micro-emulsifying drug delivery system (S-SMEDDS) of Dolutegravir for enhanced solubility and dissolution behaviour. Initially, solubility of DG was checked to select oil, surfactant, and co-surfactant. Pseudo ternary phase diagram was constructed to identify microemulsion region. Liquid SMEDDS of DG were prepared using Campul MCM, Tween 80 and Transcutol P as oil, surfactant, and co-surfactant, respectively. The effect of different oil, surfactant and co-surfactant concentrations on particle size, zeta potential and %transmittance was studied using Box–Behnken factorial design. The obtained liquid SMEDDS was evaluated for its thermodynamic stability, globule size, robustness to dilution, viscosity, dye solubilization test, cloud point, etc. Satisfactory formulations of liquid SMEDDS were converted to solid form by adsorption technique using Neusilin US2 as a solid carrier. Evaluation of S-SMEDDS showed that solubility of DG in S-SMEDDS increases from 0.270 to 33.52 mg/mL. In-vitro drug release of S-DG4 showed 99.86 ± 1.47% drug release within 120 minutes while plain DG showed 32.55 ± 1.52%. Hence study revealed that S-SMEDDS is a promising approach to enhance solubility, dissolution and hence bioavailability of poorly aqueous soluble drug like DG.

Neusilin US2 based Liquisolid Compact technique for the enhancement of solubility and dissolution rate of Olmesartan: Box-Behnken design approach

Neusilin US2 based Liquisolid Compact technique for the enhancement of solubility and dissolution rate of Olmesartan: Box-Behnken design approach

Neusilin US2 based Liquisolid Compact technique for the enhancement of solubility and dissolution rate of Olmesartan: Box-Behnken design approach

Neusilin US2 based Liquisolid Compact technique for the enhancement of solubility and dissolution rate of Olmesartan: Box-Behnken design approach

Design and optimization of liquisolid compact based vaginal sustained release tablet of antifungal agent for vaginal candidiasis

Antifungal therapy is causing an alarming drug resistance problem during the treatment of Vaginal Candidiasis and also many of the antifungal vaginal marketed formulations have reported major side-effect of the irritation. Hence the quest for natural therapy is currently booming. Lawsone is having poor aqueous solubility and its antifungal activity is therefore hindered. Therefore, the present research work aimed to formulate the liquisolid compact based vaginal tablet of Lawsone to improve its solubility and dissolution rate. The tablet was optimized by 32 full factorial design. The independent factors selected were carrier (Neusilin US2): coating material (Aerosil 200) ratio (R) and concentration of the mucoadhesive polymer (HPMC K4M) while the dependent factors studied were in vitro release (6 h and 12 h) and mucoadhesive strength. The drug was dispersed in nonvolatile solvent (polyethylene glycol 400) to prepare the liquid medicament that was further used for liquisolid compact. The FTIR, DSC and XRD studies revealed no incompatibility between Lawsone and the excipients of the tablet and suggested that the drug was dispersed completely into the liquid medication and therefore transformed from crystalline to amorphous state. In vitro release study suggested sustained release with enhanced dissolution of optimized liquisolid compact tablet LT7 (94.92%) than the plain tablet (61.16%). The in vitro antifungal activity against C. albicans, C. glabrata and C. krusei for liquisolid tablet and the marketed tablet formulation showed insignificant difference.

Investigation of hot melt extrusion process parameters on solubility and tabletability of atorvastatin calcium in presence of Neusilin® US2

Reports in the literature indicate that hot-melt extrusion (HME) processing techniques could alter the mechanical properties of the pharmaceutical physical blend, which may alter successful processing during tableting. The aim of this study was to evaluate whether HME processing conditions have an impact on the tabletability of Atorvastatin calcium trihydrate (ATR) in the presence of Neusilin® US2 (NUS2). ATR drug load of 25% was mixed with 75% of NUS2 and extruded using two screw configurations, screw speeds, and feed rates. Solid-state thermal analysis showed that ATR transformed to an amorphous form which led to improved solubility. ATR tabletability was affected positively by screw configuration that had no shearing and mixing force. SEM analysis indicated that a conveying screw configuration preserved the spherical nature of NUS2, thus improving ATR tabletability. This novel study demonstrates the significance of changing and monitoring the HME process parameters, which impact the materials’ mechanical properties and may prevent adverse outcomes during tableting.

Formulation And Evaluation Of Sertraline Hydrochloride Tablet By Self Micro-Emulsifying Drug Delivery System For Solubility Enhancement

The purpose of this research is to design and formulate the Self-micro emulsifying drug delivery system (SMEDDS) of poorly water-soluble drug Sertraline Hydrochloride (SRT). SRT is commonly used selective serotonin reuptake inhibitor for the management of a number of depressive disorders. Its applicability is limited because of extensive metabolism and poor oral bioavailability of 44 %. Solubility of SRT in different vehicles is determined with the help of which ternary phase diagrams were constructed. Capmul MCM C8 EP (as oil phase), Cremophore RH 40 (as surfactant) and Labrafil M 2125 CS (as co-surfactant) were selected for development of liquid (SMEDDS) formulation. The prepared system was characterized for globule size, TEM, transmittance study, stability analysis and permeability. The formulation was converted to solid by adsorption on Neusilin US2 to convert the system into tablet the most convenient route. Results of evaluation and characterization of formulated T SMEDDS of SRT were compared with those of pure drug. In-vitro dissolution study and comparison to that of marketed formulation indicates that Tablet of this formulation helps to improve the solubility.

Fabrication and Evaluation of Solid Self Emulsifying Drug Delivery System of Dolutegravir sodium by using Adsorption to Solid Carrier Techniques

The objective of this work was to design and characterize liquid and solid self-emulsifying drug delivery systems (SEDDS) for poorly soluble Dolutegravir Sodium. To optimize the composition of liquid Dolutegravir Sodium-SEDDS, solubility tests, pseudoternary phase diagrams, emulsification studies and other in vitro examinations (thermodynamic stability, droplet size and zeta potential analysis) were performed. The central composite design was employed to optimize the formulation variables, Capmul MCM (oil), Tween 80 (surfactant) and Propylene glycol (co-surfactant). Liquid self-emulsifying drug delivery system was appraised for determination of self emulsifying time, globule size and drug release. TEM study confirmed the uniform oil globules of the optimized liquid formulation. The optimized liquid formulation was formulated into free-flowing powder (S-SEDDS) by adsorption on the materials like Aerosil 200, Neusilin US2 and compressed into tablets. The solid state characterization of S-SEDDS powder was performed by using DSC, PXRD and SEM to investigate the physical nature of the drug. Further, the accelerated stability studies for 6 months revealed that S-SEDDS of Dolutegravir Sodium was found to be stable without any significant change in physico-chemical properties. S-SEDDS of Dolutegravir Sodium with improved dissolution profile was successfully prepared by using Neusilin US2 as an adsorbent carrier as compared to marketed sample.

Development and exploration on flowability of solid self-nanoemulsifying drug delivery system of morin hydrate

• Solid SNEDDS of MH was prepared by physical adsorption method. • Flowability of solid SNEDDS was investigated by powder flow tester. • Solid state characterization confers transformation of crystalline to amorphous. • In vitro- In vivo studies revealed an improvement of dissolution & bioavailability. • The estimated shelf life of solid SNEDDS of MH was found to be 27.57 months. Morin hydrate (MH) is a promising flavonoid with diverse biological activities; unfortunately, it finds limited clinical application due to its low water solubility. Herein, we developed a liquid self nano-emulsifying drug delivery system ( l -SNEDDS) employing Labrafil M 1994 CS, Cremophor RH 40, and Transcutol HP. The l -SNEDDS has been solidified by physical adsorption using inert carriers, i.e., Neusilin US2 and Aerosil 200. The S-SNEDDS was thoroughly investigated for flow function (FF), effective angle of wall friction (EAWF), and effective angle of internal friction (EAIF) employing a powder flow tester (PFT). The solid-state characterizations of S-SNEDDS were performed using FTIR, DSC, PXRD, and SEM. Further, in vitro dissolution, in vivo pharmacokinetic, and shelf life estimation were performed on selected SOF-2 formulation. The SOF-2 reveals good emulsifying ability, particle size (52 ± 4.25 nm), and PDI (0.133 ± 0.06). The FF and Jenike’s classification suggests the “free-flowing” nature of S-SNEDDS prepared using Neusilin US2. Further, S-SNEDDS prepared using Neusilin US2 showed a low friction angle, i.e., EAWF and EAIF, than Aerosil 200, therefore, a better flowability. The solid-state characterization of SOF-2 demonstrated the transition of MH from crystalline to amorphous state and good compatibility between MH and Neusilin US2. Further, SOF-2 showed more dissolution than pure MH and subsequently 2.97-fold increments in its oral bioavailability. Moreover, the shelf life of SOF-2 was reported to be 27.57 months, suggesting its excellent physical and chemical stability. In brief, solidifying l -SNEDDS and investigating flow behaviors by PFT could find attention in the pharmaceutical and food industry for commercial purposes.

Solid Self-Nano Emulsifying Nanoplatform Loaded with Tamoxifen and Resveratrol for Treatment of Breast Cancer.

The solid self-nanoemulsifying drug delivery system (s-SNEDDS) is a growing platform for the delivery of drugs via oral route. In the present work, tamoxifen (TAM) was loaded in SNEDDS with resveratrol (RES), which is a potent chemotherapeutic, antioxidant, anti-inflammatory and P-gp inhibitor for enhancing bioavailability and to obtain synergistic anti-cancer effect against breast cancer. SNEDDS were developed using capmul MCM as oil, Tween 80 as surfactant and transcutol-HP as co-surfactant and optimized by central composite rotatable design. Neusilin US2 concentration was optimized for adsorption of liquid SNEDDS to prepare s-SNEDDS. The developed formulation was characterized and investigated for various in vitro and cell line comparative studies. Optimized TAM-RES-s-SNEDDS showed spherical droplets of a size less than 200 nm. In all in vitro studies, TAM-RES-s-SNEDDS showed significantly improved (p ˂ 0.05) release and permeation across the dialysis membrane and intestinal lumen. Moreover, TAM-RES-s-SNEDDS possessed significantly greater therapeutic efficacy (p < 0.05) and better internalization on the MCF-7 cell line as compared to the conventional formulation. Additionally, oral bioavailability of TAM from SNEDDS was 1.63 folds significantly higher (p < 0.05) than that of combination suspension and 4.16 folds significantly higher (p < 0.05) than TAM suspension. Thus, findings suggest that TAM- RES-s-SNEDDS can be the future delivery system that potentially delivers both drugs to cancer cells for better treatment.

Development and Optimization of Vitamin D3 Solid Self-Microemulsifying Drug Delivery System: Investigation of Flowability and Shelf Life.

We report herein the design of a solid self-microemulsifying drug delivery system (SMEDDS) of vitamin D3 for augmentation of its solubility and dissolution. The studies employed a 32 full factorial design by employing JMP 13.2.1, software for preparation of liquid SMEDDS. Further, the prediction profiler was utilized to optimized liquid SMEDDS-Vit.D3 (OF) formulation. The solidification of liquid SMEDDS-Vit.D3 formulation was carried out by physical adsorption over Neusilin US2 and Aerosil 200 carriers. Solid-state evaluation of SMEDDS-Vit.D3 suggested the transformation of crystalline to amorphous form of Vit.D3 which is responsible for imparting more aqueous solubility and thus enhancement in dissolution behaviour. The investigation of flow behaviours viz. flow function (FF) and effective angle of wall friction (EAWF) of solid SMEDDS-Vit.D3 was performed using powder flow tester. Solid SMEDDS-Vit.D3 prepared using Neusilin US2 showed good flow behaviour and hence was developed into tablets. The tablets showed good quality control parameters as per pharmacopeial standards. The in vitro dissolution studies demonstrated more dissolution of Vit.D3 in SMEDDS (liquid, solid, and tablet) when compared to the unprocessed drug. The shelf life (T90) of tablets was reported to be 28.12 months suggesting excellent stability of Vit.D3 in solid SMEDDS. In nutshell, our research works explore the utilization of SMEDDS for the oral delivery of Vit.D3 to gain maximum health-related benefits.

Preparation and Characterization of Advanced Nano medicine For Malaria: Box Behnken Design Approach

In tropical countries, malaria is a larger cause of sickness and death in adults and children. Drug resistance with antimalarial therapy has now become a serious problem worldwide and it is the basic reason for the need of combination therapy. Artemisinin-based combination therapy (ACT) is widely used nowadays. The drugs selected for the study from ACT were an Artesunate (AST) and Lumefantrine (LUM). In this study, the optimized Solid-Self nanoemulsifying drug delivery system (S-SNEDDS) formulation of AST and LUM was developed using Box Behnken design (BBD) which showed greater in-vitro drug release when compared to marketed formulation. Both the drugs AST and LUM show high solubility in Anise oil, Tween 80 (surfactant), and PEG 400 (co-surfactant). Ternary phase diagrams were used to select nanoemulsifying regions. It was found to have a maximum nanoemulsion region with a 2:1 surfactant to co-surfactant ratio. The effect of formulation variables was studied by BBD. Thirteen formulations were prepared and were further characterized based on globule size, PDI, zeta potential, self-emulsification time, cloud point, % transmittance and in vitro dissolution profiles. The optimized Liquid-SNEDDS (L-SNEDDS) with RHLB 13.76 gives globule size (82.8 nm), % T (96.7 %), in vitro release of AST (98.4 %) and LUM (97.07%) at 45 min. was converted into S-SNEDDS by using neusilin US2 as an adsorbent. The S-SNEDDS was characterized by SEM, globule size (98.24 nm), % T (95.02 %), in vitro release of ART (95.18 %) and LUM (96.4%) at 45 min. DSC and FTIR study for S-SNEDDS assure that there was an absence of any chemical interaction within the drug and carrier. SEM, X-ray diffraction studies confirmed that drugs exist in amorphous nature. The present research successfully developed S-SNEDDS for bioavailability enhancement of AST and LUM in fix dose combination&#x0D;