Cumulative Percentage Drug Release Research Articles

A COMPARATIVE ASSESSMENT OF VESICULAR FORMULATIONS: TRANSFERSOMES AND CONVENTIONAL LIPOSOMES LOADED IVABRADINE HYDROCHLORIDE

Objective: Ivabradine hydrochloride (IH), a benzazepine derivative used to treat cardiovascular disease angina pectoris. In this study IH-loaded novel carrier systems transfersomes (TFs) and conventional liposomes (CLs) were developed and compared for their efficacy to enhance the stability of drugs from degradation.
 Methods: TFs formulations (TF-1, TF-2 and TF-3) were prepared by using different biocompatible surfactants; tween-80 (TW), span-80(S) and sodium deoxycholate (SC) in the concentration ratio of 15 parts with 85 parts of soy phosphatidylcholine as phospholipid by thin-film hydration method. These vesicles were compared with CLs formulation (L-1) prepared in 7:3 molar ratio of soy phosphatidylcholine: cholesterol by following the same method. These vesicles were compared for physical appearance, vesicle shape, and size, percentage drug entrapment efficiency (%DEE), deformability index (DI), in vitro percentage cumulative drug release study, and physical stability studies. The chosen optimized novel carriers were observed under scanning electron microscopy.
 Results: The compared data demonstrated that the physical appearance for all vesicles was turbid and had a spherical shape. The size distribution was in the range of 129.0 nm to 273.5 nm in vesicles. The %DEE (79.0±0.94) and DI (35.0±1.9) was found maximum in TF-1 formulation that was 2.3 times higher than L-1 formulation. The in vitro percentage cumulative drug release study followed second-order polynomial kinetics that was 2.0 times higher than L-1and 2.9 times higher than the plain drug in 30 min (90.4±0.06%) from TF-1. The vesicles were found to be stable at refrigeration conditions.
 Conclusion: Thus, amongst of all vesicles TW loaded TFs (TF-1) was chosen as an excellent novel vesicular carrier for hydrophilic drugs due to its higher deformability behavior than CLs that protects the certain drugs from biodegradation and provides stability.

Graphene oxide reinforced nanocomposite oleogels improves corneal permeation of drugs

The research on ocular drug delivery (ODD) has attracted a continual interest of researchers in the last decade. Herein, we propose to develop oleogel-based formulations for ODD applications. A series of novel nanocomposite oleogels of groundnut oil (GNO) and stearic acid (SA) were prepared, which contained graphene oxide (GO) in the concentration range of 0.00 wt% and 0.05 wt%. The pristine oleogel appeared yellowish-white. However, an increment in the GO content correspondingly imparted a black color hue to the oleogels. Confocal microscopy suggested a considerable branching of the fibrillar network of the fat crystals at lower concentrations of GO. FTIR spectroscopy revealed that GO did not tailor the interactions among the functional groups that are present within the different components of the oleogels. The X-ray diffraction study suggested that the oleogel with the highest GO content was the most crystalline in nature and had a low lattice strain. The mechanical stability of the oleogels was significantly increased when the GO concentration was >0.015 wt%. Thermal analysis of the oleogels confirmed the crystallization of SA in different polymorphic forms. Furthermore, the thermal stability of the fat network structure was higher in the nanocomposite oleogels. The rate of crystallization of SA was higher in the GO-containing oleogels. In general, the in vitro release and ex vivo corneal permeation of the model antibacterial drug (Ciprofloxacin HCl) from the prepared oleogels was Fickian diffusion mediated. Oleogel that contained 0.015% of GO exhibited a ~2.00 fold increase in the cumulative percentage of drug release. The cumulative percentage of drug permeation through caprine cornea was increased by ~2.00 folds in the oleogel that contained 0.05% of GO. The prepared oleogels were cytocompatible with human mesenchymal stem cells. The drug-loaded oleogels showed good bactericidal activity against E. coli. In conclusion, GNO/SA/GO-based nanocomposite oleogels were found to have the potential to be explored for ODD applications.

Application of Simple Lattice Design and Desirability Function for Formulating and Optimizing SMEDDS of Clofazimine

Clofazimine displays high intersubject variability in absorption after oral administration because of its extremely low water solubility and high lipophilicity. The present investigation was aimed to prepare self micro emulsifying drug delivery system (SMEDDS) of clofazimine for improving its dissolution properties by using design of experiment (DoE) approach. Various lipid, surfactant, and co-surfactants were screened based on their ability to solubilize clofazimine and their ability to make a clear transparent microemulsion upon dilution with water. Based on these tests, Capmul MCM, Tween-20, and Labrasol were selected as lipid, surfactant, and co-surfactant respectively. The design batches were prepared according to simplex lattice design and the optimized batch was selected by using the desirability function of design expert software. Contour plots and response surface plots were generated to understand the effect changed in formulation composition on critical product parameters (globule size and cumulative percentage drug release in 30 min). All the prepared batches released more than 85% drug in less than 60 min in 1.2 pH HCl and 6.8 Phosphate buffer. The validity of the model was proved by observed close agreement between the experimentally obtained values for optimized batch and predicted values given by the polynomial equation. The present investigation successfully demonstrated the effectiveness of the simplex lattice design and desirability function for optimizing the SMEDDS formulation and its ability to explain the effects of formulation variables on critical product attributes.

Ionic Liquid Drug-based Polymeric Matrices for Transdermal Delivery of Lidocaine and Diclofenac

This work prepared and evaluated transdermal patches for delivery of lidocaine and diclofenac. Pectin and Eudragit® NE 30 D were used as a polymer matrix, and glycerin was used as a plasticizer. A lidocaine–diclofenac ionic liquid drug was prepared by ion-pair reactions between the hydrochloride salts of lidocaine and the sodium salts of diclofenac. Characterization properties of blank films and transdermal patches such as mechanical properties, differential scanning calorimeter, thermogravimetric analysis, X-ray diffraction, and scanning electron microscope were evaluated, and the in vitro drug release was studied. It was found that the amount of Eudragit® NE 30 D and the lidocaine–diclofenac ionic liquid drug loading directly affected all characterization properties. Moreover, the crystal characteristics of the drug were found in the transdermal patches when the amount of Eudragit® NE 30 D increased. The thicknesses of the blank films and transdermal patches were in the range of 193–231 µm and 200–233 µm, respectively. The drug contents in transdermal patches were in the range of 1.88–2.11 mg/cm2 and 2.33–2.64 mg/cm2 for lidocaine and diclofenac, respectively. The drug release values of both lidocaine and diclofenac were controlled by the polymer matrix of the transdermal patches. However, the percentage of cumulative drug release decreased when the crystals were in the transdermal patches. In conclusion, the preparation of ionic liquid drug-based polymeric matrices for transdermal delivery of lidocaine and diclofenac provided controlled drug release and will be developed in future studies.

Development and Characterization of Biocompatible Mannose Functionalized Mesospheres: an Effective Chemotherapeutic Approach for Lung Cancer Targeting.

The aim of the present study was to analyze the lung targeting potential of surface engineered mesospheres loaded with doxorubicin hydrochloride (DOX). Gelatin-based DOX encapsulated mesospheres were prepared using a steric stabilization process and surface modified with mannose, using the amino group present on the surface of the mesospheres. Gelatin-DOX-mesospheres (M1) and gelatin-mannosylated-DOX-mesospheres (M2) were characterized for particle size, polydispersity index, zeta potential, and % entrapment efficiency which were found respectively 8.7 ± 0.35, 0.671 ± 0.018, 1.74 ± 0.27, and 80.4 ± 1.2 for (M1) and 9.8 ± 0.41, 0.625 ± 0.010, 0.85 ± 0.11, and 75.1 ± 0.7 for (M2). Furthermore, the mesospheres were characterized by FTIR, DSC, SEM, and TEM. In vitro drug release study of optimized formulation was carried out using the dialysis tube method. The cumulative percent drug release was found to be 79.2 ± 0.1% and 69.6 ± 0.52% respectively for gelatin-DOX-mesospheres and gelatin-mannosylated-DOX-mesospheres. In vitro cytotoxicity of formulations was determined using xenograft A-549 tumor cell lines. The cytotoxicity recorded as IC50 was more in the case of M2 compared to M1. In addition, mesospheres exhibited minimal hemolytic toxicity and appear to be promising for sustained drug delivery of DOX to the lungs. Cytotoxicity assay was conducted on the A-549 cell line. The results revealed that gelatin-mannosylated-DOX-mesospheres were maximally cytotoxic as compared to free DOX as well as gelatin-DOX-mesospheres. The lung's accumulation of drug was measured and found maximum after administration of M2. It may, therefore, be inferred that gelatin-mannosylated-DOX-mesospheres are capable to carry bioactive(s) and can be used specifically to target the lung cancer with minimal side effects.

Microsponge Based Gel of Tea Tree Oil for Dermatological Microbial Infections

Objective: Tea Tree Oil (TTO), derived from Melaleuca alternifolia possesses broad spectrum antimicrobial potential. However, its therapeutic utility is impaired due to its high volatility, poor aqueous solubility and low stability in the presence of light, oxygen and temperature. The present study was attempted to investigate Ethyl Cellulose (EC) microsponges (MSs) as topical carriers for TTO to circumvent above mentioned limitations. Methods: TTO MSs were prepared using quasi emulsion solvent diffusion technique. The effect of formulation variables on the production yield, entrapment efficiency, particle size and drug release of MSs was investigated. The optimized MSs were dispersed into Carbopol 934 gel and evaluated for drug release, skin irritation, antibacterial activity and photostability. Results: Scanning electron microscopy revealed spherical and porous nature of TTO microsponges. The optimized MSs possessed particle size of 36.98 μm, percent entrapment efficiency of 93.12% and percent cumulative drug release of 79.18%, respectively. MS-loaded gels were found nonirritant. In addition, TTO loaded MS gels exhibited good stability. Antimicrobial effect of TTO MS gel showed broader zones of inhibition in comparison to TTO gel. Conclusion: The findings of our study suggest that MS loaded gel could prove alternative to conventional antibacterial formulations for dermatological microbial infections.

6-Mercaptopurine Loaded Mesoporous Silica Nanoparticles as Sustained Drug Delivery for Cancer

Hollow mesoporous silica nanoparticles were successfully fabricated and functionalized, and all functionalized hollow mesoporous silica nanoparticles maintained 150 μm particle size and 8 nm pore size. The loading capacity of the hollow mesoporous silica nanoparticles to the anticancer drug, 6-MP, can be controlled via precise functionalization and concentration during the formulation. The formulation F1, F2, F3, F4, and F5 showed the drug entrapment with values of 35.87, 32.95, 63.42, 48.22, and 57.53%, respectively. The presence of amine groups on the surface of nanoparticles resulted in the highest loading capacity of 63.42%, due to the amine functionalized nanoparticles having a similar hydrophilicity but reverse charge to the drug. The percentage cumulative drug release of the formulations F1, F2, F3, F4, and F5 were optimized according to drug entrapment efficiency. The drug release was performed for 20 h, which were found to be 78.97%, 74.49%, 92.05%, 70.13%, and 83.72%, respectively. The loaded MSNs were shown to release the drug for more than 20 h and thus sustained the release. The % tumor growth inhibitions (TGI) that were found for formulations 6-MP, F1, F2, F3, F4, and F5 were 10.3, 12.4, 14.92, 25.42, 17.56, and 21.71%, respectively. The prepared formulation F3 showed the most excellent effect and maximum percentage TGI effect to comparison with other formulations due to high drug entrapment and better drug release from the formulation. The enhanced drug entrapment to hollow MSNs has demonstrated that it can become potential intracellular delivery of 6-MP for antitumor agents.

Tailoring of Colon Targeting with Sodium Alginate‐Assam Bora Rice Starch Based Multi Particulate System Containing Naproxen

AbstractThis research is focused on the formulation and optimization of Assam Bora rice starch (ABRS)‐alginate beads containing a non‐steroidal anti‐inflammatory drug (NSAID) such as Naproxen (NA), by an ionotropic gelation technique using 32 factorial design for colon targeting against rheumatoid arthritis, inflammatory bowel disease, and colon cancer. The impact of a polymeric blend of sodium alginate (SA) and ABRS on the drug entrapment efficiency (DEE, %), bead size (BS), and percentage cumulative drug release in the first 6 h (Q6, %) is optimized. The DEE (%) of all the developed beads is found to be in between 45.25% and 85.14% with an in vitro drug release of 32.81–42.18% in first 6 h. The optimized batches of beads are coated with Eudragit S100 (ES100) (5%, 10%, and 15% w/v) to facilitate colon targeting in a prominent way. The average size of the developed beads is found to be within the range of 751.61–822.22 µm. The optimized ABRS‐alginate beads containing NA show significant drug permeability over a prolonged period on ex vivo permeability through a goat colon. The in vivo roentgenographic study on rats shows the colon targeting of the beads without degradation.

Analytical method development and validation of reverse-phase high-performance liquid chromatography (RP-HPLC) method for simultaneous quantifications of quercetin and piperine in dual-drug loaded nanostructured lipid carriers

Quercetin and piperine are often used as an add-on therapy for various diseases, however both drug exhibits poor aqueous solubility and photosensitivity issue. Therefore, the aim of the present study is to improve the pharmaceutical challenges by incorporating both the drugs in nanostructured lipid carriers (NLCs) and to develop a sensitive, selective, accurate and precise reverse-phase high performance liquid chromatography (RP-HPLC) method for the simultaneous analysis of both drugs in NLCs. Effective chromatographic separation of quercetin and piperine was achieved on Hypersil gold C-18 column and mobile phase consisting of a mixture of acetonitrile and HPLC grade water (pH 2.6, adjusted with 2%v/v glacial acetic acid) in an isocratic elution mode. The flow rate of the mobile phase was 1 mL/min, column temperature at 35 ± 0.2 °C and the injection volume was 20 μL. The retention time for quercetin and piperine were found to be at 2.80 min and 10.36 min, respectively and detected at an isobestic wavelength of 346 nm using a photodiode array (PDA) detector. The method was found to be specific for the simultaneous analysis of quercetin and piperine in presence of NLCs matrix, accurate (>90%) and precise (%RSD < 2%). The validated RP-HPLC method effectively utilised to determine the percentage drug entrapment efficiency cum percentage drug loading of quercetin and piperine in NLCs enriched formulations along with the secondary estimation of in vitro cumulative percentage drug release study. The results were found to be reliable, hence the validated RP-HPLC method could be further used for the simultaneous detection and quantification of both these drugs in other lipid-based nano-formulations such as solid-lipid nanoparticles, polymer-lipid hybrid nanoparticles, lipid drug conjugates, etc. in in vitro and in vivo.

Does the Addition of Poly(glycolide-co-lactide) to Teicoplanin-Containing Poly(methyl methacrylate) Beads Change the Elution Characteristics?

The objective of our study was to measure and compare the elution characteristics of teicoplanin from poly(methyl methacrylate) PMMA beads with those of poly(glycolide-co-lactide) PGLA-added beads. The study included two groups of PMMA + teicoplanin beads. PMMA was added to teicoplanin in Group 1 and PMMA + PGLA was added to teicoplanin in Group 2. A total of 16 beads of 1 cm3 were created for each group. Samples were added individually to tubes containing 3ml of phosphate-buffered saline (PBS). Antibiotic elution was measured by measuring absorbance values of 1-ml samples taken at regular intervals using a UV-Vis spectrophotometer and cumulative percentages of drug release were calculated. In addition, the spectra of teicoplanin were identified using a FTIR spectrophotometer in a wavelength range of 400-4000cm-1. Drug elution in the PBS medium was measured and compared for Groups 1 and 2. The cumulative percentage of drug release from the PGLA-added beads (Group 2) was significantly higher (p = 0.01). The molecular structure of teicoplanin was also confirmed using FTIR. The in vitro results showed that the addition of biodegradable PGLA into bone cement functions as a water-soluble porogen which allows for significant increases in the elution of teicoplanin from cement. This increase in elution suggests that the PGLA would allow for further fluid contact and exchange with the previously entrapped drug. These results may have important clinical applications.

Development and Evaluation of Manidipine Loaded SelfNanoemulsifying Drug Delivery System by Box-Behnken Design

The current study aims to formulate an anti-hypertensive drug manidipine self-nanoemulsifying drug delivery system (SNEDDS) employing different novel polymers to enhance solubility and drug release manidipine. The optimal concentration of excipients chosen based on solubility study further confirmed by self-emulsification region of pseudo ternary phase diagram. Manidipine SNEDDS optimized employing box-behnken design (BBD) through the study of factors - the amount of capryol 90(A), cremophor RH40 (B) and triacetin (C) and responses -droplet size (Y1), zeta potential (Y2), and cumulative percentage of drug release after 60 minutes (Y3). All formulations were evaluated for particle size, zeta potential, polydispersity index, entrapment efficiency, drug content, and in-vitro drug release. The optimized formulation was characterized for FTIR, SEM, and stability studies. The study indicates that manidipine optimized formulation MF11 comprising of capryol 90 (40.0%), cremophor RH40 (10.0%) and triacetin (30.0%) exhibited minimum droplet size (76.5 ± 2.87), best zeta potential (-24.7 ± 1.31mV) and entrapment efficiency (98.23 ± 1.74%) content uniformity (99.12 ± 1.28%) maximum drug release (98.79 ± 1.68%). The fourier transform infrared spectroscopy (FTIR) studies of MF11 indicated no significant interaction amid the drug and formulation excipients. The scanning electron microscopy (SEM) data revealed that particle size is in the nanometer range with a zeta potential value &gt;5 mV indicating higher absorption and stability. Accelerated stability studies indicated the formulation to be stable for 3 months. Hence the results revealed that application of SNEDDS formulation technique for manidipine increased solubility and drug release.

In vitro and in vivo evaluation of gentamicin sulphate-loaded PLGA nanoparticle-based film for the treatment of surgical site infection

The study focuses on the in vitro and in vivo evaluation of the developed gentamicin sulphate (GS)-loaded poly lactic-co-glycolic acid (PLGA) nanoparticle (PNP)-based pullulan film (PNP-F). Sterilization being an essential pre-requisite for the dosage form was carried out using ethylene oxide. Post-sterilization, PNP-F was evaluated for mechanical properties, percentage drug loading, antimicrobial effectiveness study, test for sterility and in vitro dissolution study using Strat-M® membrane. In vitro dissolution study revealed that GS gradually released from PNP-F and the highest cumulative percentage drug release was found to be 86.76 ± 0.03% at 192h. Wound healing assay was performed to study the effect of PNP-F over migratory potential of dermal fibroblast cells (NIH-3T3) in the presence of micro-organisms, Pseudomonas aeruginosa (PA) and Staphylococcus aureus (SA). PNP-F inhibited the growth of PA and SA, allowing the growth of fibroblast cells indicating its suitability for application. In vivo study of surgical site was performed by superficial incision model in Wistar rats. Measurement of in vivo incision healing confirmed faster wound healing in the incision which received PNP-F compared to marketed cream containing GS. Graphical abstract.

Comparison of In-Vitro Dissolution of Griseofulvin Tablet made from Nano Particles and Solid Dispersion

Objectives: To find out the comparison of dissolution results of griseofulvin tablets made from nanoparticles, solid dispersions, and conventional materials.&#x0D; Interventions: Different types of active ingredients in the form of nanoparticles and solid dispersions can affect the dissolution results of tablets.&#x0D; Main outcomes measure: The results obtained in this study are the cumulative dissolution percentage and the order kinetics of the release of active ingredients.&#x0D; Conclusion: There was no significant cumulative percent drug release difference (p&gt; 0.05) between nano particles, solid dispersions, and conventional materials. Tablets containing active nanoparticles, solid dispersions, and conventional materials show a linear relationship with a correlation coefficient (R2) close to 1, shown in zero-order kinetics models.&#x0D; &#x0D;

Preparation, Physicochemical Characterization and In-Vitro Dissolution Studies of Ketoprofen Solid Dispersion with PEG 6000 and HPMC 6 cps

Ketoprofen [2-(3-benzoylphenyl)-propionic acid], a non-steroidal anti-inflammatory drug exhibits poor dissolution pattern. Solid dispersion (SD) techniques were used because it is particularly promising to improve the oral absorption and bioavailability of BCS Class II drugs. This investigation entails solid dispersion of ketoprofen which was formulated and characterized for better release profile and immediate action of the drug. Melting method was applied to prepare solid dispersion by using two immediate release (IR) polymer PEG 6000 and HPMC 6 cps at different weight ratios. In the formulation, a fixed amount of lactose was used as adsorbent. The solid dispersions were investigated for drug entrapment efficiency and dissolution behavior. In vitro dissolution study was performed in phosphate buffer (pH 7.4) medium for one hour. Percent cumulative drug release from solid dispersion was found to be minimum 92.19% and maximum 98.95% within one hour, which showed a better dissolution compared to the active drugs. Evaluation of the properties of the solid dispersion was also performed by using Scanning Electron Microscopy (SEM) study and Differential Thermal Analysis (DTA). SEM results indicated that ketoprofen crystallinity in SDs was significantly reduced, and that the majority of ketoprofen was in amorphous form. No interaction was found between drug and polymers from DTA and Fourier-transform infrared (FTIR) spectroscopy analysis. So, solid dispersion technique may be an effective technique to enhance dissolution rate of ketoprofen. Bangladesh Pharmaceutical Journal 23(1): 44-53, 2020

Preparation of mucoahesive tablets of famotidine by wet granulation method and its in-vitro testing

Objective: Famotidine is a histamin H2-receptor antagonist.The aim and objective of the present work is toformulate and evaluate mucoadhesive tablets of famotidine. It is also foused on the selection of mucoadhesivepolymer &amp; its activity in various combinations &amp; ratios. The poor bioavialability &amp; shorter half-life suffice thedevelopment of controlled release mucoadhesive formulation. Method: Mucoadhesive tablets each containing 20mg of famotidine were prepared by conventional wet granulation method employing as mucoadhesive materials. A batch of 50 tablets was prepared, in each case a blend of 1 gm of famotidine with different polymers addition indifferent strengths with required 40mg lactose as diluent achieved after titration which were then grannulated along with a solvent blend if water and ethyl alcohol. Results: The flow properties of all five batches were in between fair and passable. Hardness of tablets ranged from 6.9-8.2 kg/cm2 and the percentage friability was between 0.25-0.79 %. The drug content uniformity in the mucoadhesive tablets was 96.49-104.81%. The surface pH study was within the range from 6.7-7.4. From all formulations, over 20% of the famotidine was release within first hour of dissolution study. In the present study the formulation FT04 (tragacanth &amp; HPMC ) has shown cumulative percent drug release of about 80.762% in 12 h. Conclusion: From the results we concluded that formulation containing famotidine with HPMC &amp; tragacanth has given better drug release property than the other four formulations &amp; the wash-off test has shown that this formulation (FT04) has better mucoadhesive property.

Formulation and Development of Sustained Release Pellets of Nifedipine by Fluidized Bed Processor

Recently, extended release pharmaceutical products became a very useful tool in medical practice, offering a wide range of actual and perceived advantages to the patients. Oral drug delivery is the most preferred route for the various drug molecules among all other routes of drug delivery, because ease of administration which lead to better patient compliance. So, oral extended release drug delivery system becomes a very promising approach for those drugs that are given orally but having the shorter half-life and high dosing frequency. Extended release is also providing promising way to decrease the side effect of drug by preventing the fluctuation of the therapeutic concentration of the drug in the body. Recent trends indicate that multiparticulates drug delivery systems are especially suitable for achieving extended release oral formulations with low risk of dose dumping, flexibility of blending to attain different release patterns as well as reproducible and short gastric residence time. Development of Nifedipine Sustained Release pellets by Fluidized Bed Processing technology. The different trials were formulated and evaluated for its percent Cumulative drug release, percent Swelling index and scanning electron microscopy. The release of drug from pellets depends on a variety of factors including the carrier used to form pellets and the amount of drug contained in them. In these, trial 2 is Shows better results Such as, percent Cumulative Drug Release is 84.34%, and Scanning Electron Microscopy study shows Pellets uniformities and Spherical shape particle's also less Agglomeration.

Development and Characterization of Colon-targeting 5-Fluorouracil Multiparticulate Beads

This investigation is related to the development and optimization of multiparticulate beads of fenugreek seed mucilage-sodium alginate containing 5-flurouracil through ionotropic gelation technique using 32 full factorial design generated with Design-Expert® Version11 software. The beads were developed using CaCl2 as the crosslinking agent. The effect of ratio of fenugreek seed mucilage and sodium alginate blend and concentration of CaCl2 on the drug encapsulation efficiency, bead size and percent cumulative drug release in 6 h was optimized by 32 factorial design. The beads were also characterized using field emission scanning electron microscopy, Fourier-transform infrared spectroscopy and thermal analysis. The percent drug encapsulation efficiency of all these beads was within the range of 43.91 to 85.39 % with an in vitro drug release of 33.92 to 39.23 % in 6 h. The optimized batches of beads were coated with Eudragit S100 (5, 10 and 15 % w/v) to facilitate colon targeting in a prominent way. The in vitro drug release from the coated beads (P3) in various colonic fluids followed zero-order pattern with erosion mechanism in 18 h. The average size of these beads was within the range of 895 to 1021 μm. The optimized fenugreek seed mucilage-alginate beads containing 5-flurouracil showed significant drug permeability over a prolonged period in an ex vivo permeability study through goat colon. The results indicated successful colon targeting of 5-flurouracil multiparticulate beads developed using polymeric blends containing sodium alginate and fenugreek seed mucilage in an appropriate ratio.

Formulation and evaluation of the topical ethosomal gel of melatonin to prevent UV radiation.

Clinically, melatonin (MLT) has variable oral absorption and extensive first-pass effect, making its oral mode less preferable. Ethosomes are able to permeate intact through the human skin due to its high deformability. Present study assessed topical potential of ethosomes loaded with MLT for the prevention of UV radiation. Melatonin was encapsulated using different ratios of ethanol, soya lecithin, and cholesterol. Prepared ethosomes were characterized for scanning electron microscopy (SEM), zeta potential, % entrapment efficiency (%EE), in vitro drug release kinetics. Then, optimized formulation was incorporated in gel and evaluated for viscosity, pH, extrudability, homogeneity, skin irritation study, spreadability, in vitro skin permeation study, flux, and stability. Ethosomes were spherical in structure as confirmed by SEM, and zeta potential was in range of -12.4mV to -27.4mV. %EE of the vesicles was in the range of 49.61%-78.047%. Cumulative percentage drug release from various ethosomal formulations was ranged from 64.82%-81.01%. F3 was selected as optimized formulation on the basis of highest %EE, zeta potential, and in vitro drug release. An ethosomal gel of optimized formulation F3 was prepared by using carbopol 934 and compared with plain gel formulation. G3 formulation showed pseudoplastic rheological behavior, optimum pH, spreadability and also showed maximum % in vitro drug permeation with flux 13.85μg/cm2 /hr and followed zero-order release kinetics which was good for topical drug delivery system. This research suggested that MLT loaded ethosomes can be potentially used as a topically drug delivery system.

FORMULATION DEVELOPMENT AND CHARACTERIZATION OF GASTRORETENTIVE DRUG DELIVERY SYSTEMS OF LORATADINE

Objective: The main objective of the research work is to develop a single unit non-effervescent drug delivery system of Loratadine (LTD) by direct compression process to prolong the gastric residence time (GRT).&#x0D; Methods: LTD non-effervescent tablets were prepared with different polymers like hydroxypropyl methylcellulose (HPMC) K15M, HPMC K100M (i.e.: 1:1, 1:2, 1:3) as release retardants. Glyceryl behenate (Compritol 888 ATO) and Glyceryl palmitostearate (Precirol ATO 5) were used (1:1, 1:2, 1:3) as low-density lipids to impart buoyancy for longer period.&#x0D; Results: The drug (LTD) and excipient (i.e. HPMC, low-density lipid aids, etc.,) interaction studies were carried out by Fourier Transform Infrared Spectroscopy (FTIR) and there was no likely interaction involving them. The developed LTD floating matrix tablets were characterized by pre and post-compression parameters and all results were, found within the pharmacopoeial limits. The cumulative percentage of drug release ranges from 56.87±0.25 % (F12) to 99.87±0.09 % (F2). The drug release profiles of the all formulations (F1 to F12) were subjected to various pharmacokinetic parameters and the optimized formulation (F3) followed the Korsmeyer Peppas (R2=0.996) model with non-Fickian diffusion (n&gt;0.5). The obtained data by radiographic images of F3 formulation showed the GRT is 6±0.5 h (n=3).&#x0D; Conclusion: Hence, from all evaluation studies, it was evident that F3 formulation was optimized (99.82±1.63 % drug release in 12 h).

Multiparticulate Drug Delivery System for Gastrointestinal Tuberculosis

Drug solubility poses numerous challenges in design of formulations for drugs with poor aqueous solubility. Ethionamide is an antitubercular drug belonging to biopharmaceutical classification system class II drug having less aqueous solubility. Nanosuspensions were prepared by using various solvents such as methanol, ethanol, acetone and chloroform and it was prepared using anti-solvent precipitation technique by using probe sonication. Various stabilizers such as tocopherolpolythytlene glycol succinate, polyvinylpyrrolidone and tween 80 singly or in combination were studied. A 32 factorial design was employed to study the effect of independent variables, concentration of stabilizers and stirring speed on particle size and cumulative percent drug release. The particle size of the optimized batch was 97.54 ± 8.47 nm with polydispersity index of 0.36 and zeta potential -10.1 ± 2.3 mV. The cumulative percent drug release of optimized batch was found to be 95.01 ± 1.16% in 60 min. Optimized batch was ultracentrifuged and evaluated for saturation solubility studies, stability and powder X-ray Diffraction studies. Optimized nanosuspension was loaded on Espheres by spraying in a coating pan and then coating of Eudragit controlled release polymers. The coated Espheres were evaluated for drug content, friability, scanning electron microscopy, ex-vivo permeation studies and drug release kinetics studies. The friability value for primary coated sphere was found to be 0.8 ± 0.12% and for secondary was 1% and the best fit model was found to be Korsmeyer-Peppas model which is indicative of diffusion controlled release. Ex vivo diffusion studies revealed a moderate increase in permeability.