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Abstract Background The overall objective was to prepare a highly accurate nanocarrier system of mesalamine for the treatment of ulcerative colitis with increased therapeutic efficacy and targeting. In the formulation of nanocarrier systems, optimization is a critical process for understanding nanoformulation variables and quality aspects. The goal of the present work was to determine the effect of independent variables, i.e., the concentrations of chitosan, carboxymethyl inulin (CMI), and the drug on the response variables, i.e., particle size and percent entrapment efficiency of the mesalamine-loaded nanoparticle using the Box Behnken design (BBD). The correlation between the independent and dependent variables was investigated using the Design Expert generated mathematical equations, contour, and response surface designs. Result An optimized batch was developed using the ionotropic gel method with selected independent variables (A: + 1 level, B: 0 level, C: − 1 level) and the developed nanoparticles had a particle size of 184.18 nm, zeta potential 26.54 mV, and entrapment efficiency 88.58%. The observed responses were remarkably similar to the predicted values. The morphological studies revealed that the formulated nanoparticles were spherical, and the results of the FTIR and DSC studies indicated the drug-polymer compatibility. The nanoparticle showed less than 5% release in the pH 1.2. In the colonic region (pH 7.4), more than 80 % of the medication was released after 24 h. The kinetics study showed that the Higuchi and Korsemeyer-Peppas models had R 2 values of 0.9426 and 0.9784 respectively, for the developed formulation indicating linearity, as revealed by the plots. This result justified the sustained release behavior of the formulation. Conclusion The mesalamine-loaded chitosan-CMI nanoparticle has been successfully developed using the ionotropic gelation method. The nanoparticles developed in this study were proposed to deliver the drug to its desired site. The developed nanoparticles were likely to have a small particle size with positive zeta potential and high percent drug entrapment. It could be stated from the results that BBD can be an active way for optimizing the formulation and that nanoparticles can be a potential carrier for delivering therapeutics to the colon.

Abstract Background Present investigation for research was to develop matrix-type transdermal drug delivery system of flurbiprofen (FBP) with the various ratio of matrix polymers (hydrophilic and hydrophobic), the concentration of plasticizer and natural penetration enhancer by Box–Behnken statistical design to investigate the combined outcome of selected independent variables for effective management of rheumatoid arthritis. The influence of a binary mixture of polymers, plasticizer and penetration enhancer on physicochemical considerations including thickness, tensile strength, percent elongation, weight variation, percent moisture content, percent moisture uptake, water vapour transmission rate, folding endurance, drug content, in vitro drug dissolution study and then ex vivo drug permeation study was evaluated. Results The study demonstrated that the tensile strength of films improved by matrix polymer ratio and to a slighter gradation in the rise of plasticizer and natural penetration enhancer. Ex vivo drug permeation study was accompanied via excised porcine skin as a permeation barrier in Franz diffusion cell. Ex vivo drug permeation study indicated that matrix polymer ratio (HPMC K15M:ERL100) at 3:1 and natural penetration enhancer (d-limonene) at highest concentration 7.5% w/w containing formulation FBPT7 delivered maximum flux and supplementary improved the permeation of drug. The result of the skin irritation test revealed that the developed formulation is free from any type of skin irritation effects like erythema and oedema. Conclusion Based on the findings of this research, it can be established that a well-controlled release and very effective skin penetration of the drug was accomplished by the film FBPT7 in the existence of permeation enhancers for prolonged periods.

Abstract Background Chicory is one of the major source of inulin. In our study, Box–Behnken model/response surface analysis (RSM) was used for the optimization of spray drying process variables to get the maximum inulin yield from chicory (Cichorium intybus L.). For this investigation, the investigational plan utilized three process variables drying temperature (115–125 °C), creep speed (20–24 rpm), and pressure (0.02–0.04 MPa). Result The optimal variables established by applying the Box–Behnken model were as follows: drying temperature 119.20 °C, creep speed 21.64 rpm, and pressure 0.03 MPa. The obtained powdered inulin by spray drying was investigated for the yield value, identification, size, and surface morphology of the particle. The inulin obtained from the spray drying process consists of a fine molecule-sized white powder. Instead, the drying methods shows a significant effect on the morphology and internal configuration of the powdered inulin, as the inulin obtained from spray drying was of a widespread and uniform size and shape, with a rough surface on increase in temperature and smoother surface while increasing the creep speed. The findings indicate that the spray drying with optimum parameters resulted in maximum product yield. Conclusion The outcomes of the study concluded that the product yield through spray drying technique under optimized condition is optimal as compared to other drying technique. Hence, this technique may be applied at commercial scale for the production of inulin.

Abstract Background The goal of the current investigation was to formulate, evaluate co-crystal, and further design of solid unit dosage form of antihyperlipidemic BCS class II drug fenofibrate (FNO). Co-crystals composed of a structurally homogeneous crystalline material that contains two or more components in a definite stoichiometric amount helps in increasing yield, the capability to regulator polymorph fabrication, enhanced invention crystallinity. Ball milling method is used for co-crystal formulation, optimized via 32 full factorial design and characterized by saturation solubility, particle size analysis, Fourier transform infrared spectroscopy (FT-IR) study analysis, powder X-ray diffraction (PXRD) study analysis, surface morphology by scanning electron microscopy (SEM) study, flow properties, and ex vivo intestinal permeation study via non-everted rat intestinal sac model. Furthermore, optimized batch compressed into tablets is evaluated for disintegration time, hardness, friability, in vitro drug release study and stability study. Results It demonstrated that co-crystal formulation FNOCC7 shows higher saturation solubility 0.3874 ± 2.82 g/ml with less particle size 221.231 ± 0.456 nm, FT-IR spectra confirmed significant structural alterations in the formulation indicating the hetero-molecular interaction, the presence of hydrogen bonding had occurred in the co-crystals, PXRD spectra of formulation determined by the increase in the crystalline nature. FNO co-crystals show flux (F) and permeability coefficient (P app) 0.322 ± 0.068 μg/min, 5.38 ± 0.093 cm/min respectively increased compared to the pure drug makes in an enhancement of solubility as well as the bioavailability of BCS class II drug. Conclusions The solubility and dissolution percentage of FNO can be improved by the utilization of Co-crystal of FNO with PEG 4000. The solubilization impact of PEG 4000 might be contributed because of the decrease of molecule conglomeration of the drug presence of crystallinity, expanded wettability, and dispersibility; pharmaceutical co-crystals speak to a beneficial class of crystal form with regard of pharmaceuticals.

Aim: The objective of the present study is to design and evaluate mucoadhesive microspheres for oral controlled release. Materials and Method: Rosiglitazone maleate microspheres with a coat consisting of alginate and a mucoadhesive polymer sodium carboxymethylcellulose, carbopol 934P and hydroxypropylmethylcellulose were prepared by an orifice-ionic gelation process. The microspheres were evaluated for FTIR studies, morphology, particle size, micromeritic properties, percentage entrapment efficiency, in-vitro wash-off test and in-vitro release studies. Results: The resulting microspheres were spherical and free flowing. The percent entrapment efficiency was 68.2 to 85.6%. The microspheres exhibited good mucoadhesive property in the in vitro wash-off test. Rosiglitazone release from these mucoadhesive microspheres was slow and extended over 12 h duration of time depending on the composition of coat. Conclusions: The prepared mucoadhesive microspheres are thus suitable for oral controlled release of Rosiglitazone maleate and thereby help in the management of type II diabetes mellitus.

Solid lipid nanoparticles (SLNs) of zolmitriptan were produced by solvent emulsification-diffusion technique. Soya lecithin and poloxamer 188 were used as surfactants and stabilizers of the particles. The formulations were optimized for independent variables (amount of stearic acid, amount of lecithin and homogenization time) in order to achieve desired particle size with maximum percent entrapment efficiency (% EE). Prepared SLNs were characterized by transmission electron microscopy (TEM), atomic force microscopy (AFM) and zeta potential measurements. To achieve our goal, eight formulations (F1–F8) of SLNs were prepared by solvent injection technique and optimized by 23 full-factorial design. The responses of the design were analyzed using Minitab 15. On the basis of software analysis, formulation F8 was selected as optimized formulation and was evaluated for the independent parameters. Optimized formulation showed particle size of 340nm, percent entrapment efficiency (EE) of 81.36 and 79.11% of in-vitro drug release after 24h. The release kinetics of the optimized formulation best fitted the Higuchi model.

The delivery of a drug to the preferred site of action is referred to as drug targeting. The benefits of drug targeting are a reproducible and controlled release rate of the therapeutic compound, which forestalls overdose. Due to the potential to treat colonic diseases with minimum side effects, colon targeting has become of high interest over the last decades. Inulin was investigated for its potential as encapsulation material regarding its enzymatic degradability and its drug release behaviour. Inulin is a polysaccharide with a widespread range of therapeutic uses such as a carrier in a drug delivery vehicle, as a diagnostic/analytical tool or as a dietary fibre with additional health benefits. In the main, much research has focused on inulin as a drug delivery carrier for colon-specific drug delivery. The justification for this is its potential to survive in the stomach's acidic environment. This unique stability and strength are utilized in many ways to deliver drugs safely to the colon, where they can be easily absorbed through the gut epithelium into the blood. There are also some proofs that inulin's prebiotic features also lead to health benefits, mainly for patients with inflammatory bowel disease or in the prevention of colonic cancer. Inulin based hydrodynamic research will be useful to discover the potential of inulin. [ABSTRACT FROM AUTHOR]

The present study aimed towards the development of active delivery system for management of hypertension. The Orodispersible tablets (ODTs) containing Telmisartan was developed in order to accomplish enhanced solubility leading to better bioavailability profile. Different ratios, of Telmisartan and PEG 6000 i.e. 1:1, 1:2, 1:3, 1:4 and 1:5 were selected for the formulation of ODT system. A batch process was adopted for the preparation of solid dispersion with each combination of drug and polymer and the finally compressed as tablets by direct compression technique. For the preformulation perspective materials were scrutinized on the basis of solubility profile, drug content, Fourier Transform Infrared (FTIR) spectroscopy and Differential scanning calorimetry (DSC). The drug polymer ratio 1:4 was selected for further compression process. The prepared batches of ODTs were characterized for micromeritic study, thickness, hardness, weight variation, wetting time, disintegration time, drug content and in vitro drug release profile. The evaluation data for all batches was satisfactory out of them formulation TF3 containing 6% kyron T-314 showed the best results with a value of 29.3 sec and 24.1 sec for wetting and disintegration, respectively. This formulation showed superior drug release of 99.93% over a period of 30 minutes. [ABSTRACT FROM AUTHOR]