Showed Drug Release Research Articles

FORMULATION DEVELOPMENT AND EVALUATION OF FAST DISSOLVING TABLET OF TRIPTAN DRUG

Almotriptan malate is a triptan class anti-migraine drug with rapid action, highest bioavailability and low side effects. Fast dissolving tablets of almotriptan malate were prepared by wet granulation technique using sodium starch glycolate, Crosscarmellose sodium and Crosspovidone (2%, 4%, and 6%), respectively, FT-IR spectroscopy and differential scanning calorimetry were used to investigate the physical characteristics of the drug. The granules were examined for angle of repose, bulk density, tapped density, index and Hausner’s ratio. Developed tablets were evaluated for hardness, drug content, friability, wetting time, wetting absorption ratio, in vitro drug release and disintegration time. Formulation with 4% crosspovidone showed disintegration time of 21.5 sec. In vitro dissolution studies showed drug release of 94.66% after 12 minutes. The drug release from the formulation followed zero order kinetics. The optimized formulation was found to be promising and can be considered for further study.

Nose to Brain Delivery of Midazolam Loaded PLGA Nanoparticles: In Vitro and In Vivo Investigations.

The present study is aimed to develop poly(D, L-lactide-co-glycolic acid) (PLGA) nanoparticles (NP) loaded with midazolam (Mdz) for nose to brain delivery. NP were formulated by nanoprecipitation and characterized for z-average, zeta potential, % drug entrapment and ex vivo drug release. Mdz NP (MNP) were radiolabeled with technetium-99m. Biodistribution and gamma scintigraphic studies were performed on Sprague-Dawley rats following intranasal (i.n) and intravenous (i.v) administration to trace the transport of Mdz for nose-to-brain delivery. MNP showed z-average of 164±4.5nm with polydispersity index 0.099±0.02 and zeta potential of -16.6±2.5mV. Ex vivo drug studies indicated that MNP showed 29±1.2% of permeation upto 4h via sheep nasal mucosa, whereas Mdz suspension (MS) showed drug release of 83±1.2% within 4h. Comparing i.n administration of MNP, MS and i.v administration of MS, scintigraphy imaging and Brain/blood uptake ratios indicated higher brain targeting via i.n administration of MNP. Results indicated that the i.n MNP could be employed as a non invasive mode of delivery system with improved drug entrapment, stability and controlled drug release over a period of time.

Hydrophobic ion pairing of a minocycline/Ca2+/AOT complex for preparation of drug-loaded PLGA nanoparticles with improved sustained release

Polymeric nanoparticles is an established and efficient means to achieve controlled release of drugs. Incorporation of minocycline, an antibiotic with anti-inflammatory and neuroprotective properties, into biodegradable nanoparticles may therefore provide an efficient means to combat foreign body reactions to implanted electrodes in the brain. However, minocycline is commonly associated with poor encapsulation efficiencies and/or fast release rates due to its high solubility in water. Moreover, minocycline is unstable under conditions of low and high pH, heat and exposure to light, which exacerbate the challenges of encapsulation. In this work drug loaded PLGA nanoparticles were prepared by a modified emulsification-solvent-diffusion technique and characterized for size, drug encapsulation and in vitro drug release. A novel hydrophobic ion pair complex of minocycline, Ca2+ ions and the anionic surfactant AOT was developed to protect minocycline from degradation and prolong its release. The optimized formulation resulted in particle sizes around 220nm with an entrapment efficiency of 43% and showed drug release over 30 days in artificial cerebrospinal fluid. The present results constitute a substantial increase in release time compared to what has hitherto been achieved for minocycline and indicate that such particles might provide useful for sustained drug delivery in the CNS.

Formulation and Pharmacokinetic Evaluation of Microcapsules Containing Pravastatin Sodium Using Rats.

Pravastatin Sodium has a cholesterol lowering agent. It has shorter half-life and undergoes first-pass metabolism. Frequent dose is required in case of conventional dosage form. The purpose of the study is to formulate and evaluate microcapsules containing Pravastatin Sodium by complex with cholestyramine resins coated with Eudragit RLPO and Eudragit RSPO polymers for achieving control release. Complexation of drug on resin was carried out by batch method. Microencapsulation was carried out by nonaqueous solvent evaporation method. Pharmacokinetic studies were done by using rats. The intermediate stability studies were carried out on the most satisfactory formulations. FTIR, X-ray diffraction, and DSC spectra of drug, drug-resinates, and polymers revealed no chemical interaction. The % DEE and % yield were observed for formulations of f1 to f7 that were varied from 97.1 ± 0.8 to 98.9 ± 0.5% and 95.0 ± 3.25 to 98.8 ± 7.1%, respectively. Most satisfactory formulation, f6, showed drug release up to 72.6%. No changes in % DEE and % CDR were observed after stability studies. Microcapsules of f6 formulation achieved best performance regarding in vitro drug release and from pharmacokinetic evaluation mean residence time was found to be 6.3 h, thus indicated, Pravastatin Sodium microcapsules were released and absorbed slowly over a prolonged period of time.

Formulation and Development of Ethyl cellulose coated Pectin based Capecitabine Loaded Microspheres for Colorectal Cancer

The main objective of present investigation was to design the colorectal microspheres of Capecitabine by using inexpensive natural polysaccharide based polymers. The pectin microspheres were prepared by single emulsification technique using calcium chloride as crosslinking agent. Pectin loaded microspheres were coated with ethyl cellulose by solvent evaporation method. The prepared microspheres were characterized by entrapment efficiency, particle size, in-vitro drug release, scanning electron microscopy (SEM), Fourier transform infrared spectroscopy (FTIR), and Differential scanning calorimetry (DSC). The in-vitro drug release behaviour of ethyl cellulose coated pectin microspheres done in varying pH conditions up to 12 hr. Optimized uncoated batch of pectin based capecitabine microspheres showed optimum particle size with good drug encapsulation efficiency and spherical in nature. All the formulations showed less than 20 % drug release in acidic environment. Ethyl cellulose coated microspheres mininised initial burst effect and showed drug release in the range of 85.33 to 95.55% at the end of 12h. As concentration of ethyl cellulose was increased drug release was found to be retarded well. From above results it can be concluded that capecitabine loaded ethyl cellulose coated pectin based microspheres may be the best alternative to conventional tablets to treat the colon cancer.

Preparation, Optimization and Characterization of Eudragit Coated Chitosan Piroxicam Microspheres Intended for the Treatment of Rheumatoid Arthritis

As a novel drug delivery approach, piroxicam an anti rheumatoid drug is loaded in microspheres prepared by chitosan as a polymer and coated with eudragit S-100 to prepare colon specific microspheres which increases the bioavailability of the drug to the targeted area and in a controlled manner and reduces GI related side effects. In the present study chitosan microspheres were prepared using emulsion crosslinking technique, glutaraldehyde as a crosslinker and microencapsulation using phase coacervation technique. Optimization is done by varying drugpolymer ratio (1:2 to 1:8), emulsifier concentration, i.e., span 80 (0.5 ml, 0.75 ml, 1 ml), stirring speed (500 rpm, 1000 rpm, 1500 rpm, 2000 rpm, 2500 rpm), cross-linker concentration (2.5 ml, 5 ml, 10 ml) and coat-core ratio from 1:2 to 1:6. The prepared chitosan microspheres showed high entrapment efficiency about 97.29% with percent yield 90.26. In the present study FTIR studies confirmed the absence of interactions between the pure drug, i.e., piroxicam and the excipients used. SEM images revealed that the prepared chitosan microspheres were spherical in shape with rough surface and particle size ranged from 90.21 to 172 μm. Showed good drug release profile for both coated and uncoated chitosan piroxicam microspheres of about 86% and 96%. Drug release kinetics showed that microspheres followed korsemeyer peppas model indicating the drug diffusion mechanism from polymer matrix.

Preparation and Characterization of Modified Polyethyleneimine Magnetic Nanoparticles for Cancer Drug Delivery

Magnetic nanoparticles with polymeric coating have great significance in drug delivery purpose. We intended to prepare a modified amphiphilic polymer with targeting susceptibility to reduce side effects to normal cells. In this study polyethyleneimine (PEI) as a polycationic polymer reacted with sebacoyl chloride to make a new amphiphilic polymer and folic acid as a targeting agent to reduce cytotoxicity of polymer and increase specific entrance of nanoparticles to cancerous cells. The obtained polymer (PEI-Sb-FA) was then coated on magnetic nanoparticles (MNPs) to stabilize them. The core-shell nanoparticles were characterized by different methods such as scanning electron microscopy (SEM), X-ray diffraction (XRD), thermogravimetric analysis (TGA), and vibrating sample magnetometer (VSM). Curcumin was finally loaded on PEI-Sb-FA-MNPs and the release behavior was studied in different pH. Curcumin loading of 28.2% was obtained and released drug in acidic pH = 4.5 was more than pH = 7.4, showing drug release sensitivity toward pH of media.

Formulation Development and Evaluation of Topical Film-Forming Lotion Containing Butenafine Hydrochloride

Many agents are applied to the skin deliberately with beneficial outcomes. Conventional formulations intended for topical and dermatological administration of drugs such as creams, foams, gels and lotions are considered to reside for a relatively short period of time at the targeted site. The localized treatment of body tissues, diseases and wounds requires that the particular pharmaceutical component be maintained at the site of treatment for an effective period of time. Sweat, clothing, movements and getting washed away easily on contact with water are some of the problems that have limited the effectiveness and residence time of conventional topical formulations for treatment of fungal infections of skin. This necessitates longer treatment duration. Hence, a composition that adheres to skin surface afflicted and provides localized delivery of an antifungal agent is needed. The present work aims at designing and formulating a 'film- forming lotion' which on application will form a thin transparent film on the skin. Eudragit RL 100 and HPMC K4M was used to form a matrix film. The formulations were prepared using 32 full factorial design. They were tested for drying time, drug release, antifungal activity, skin irritation and stability studies. The gel was characterised for pH, viscosity, drug content, effective dosage volume and mechanical properties of the film formed after application; bioadhesion and water vapour permeability were also tested. All the formulations showed results within acceptable range for various tests. The optimized formulation showed drug release of 99.64% and antifungal activity in terms of efficacy as 98.72%. Such a formulation can be claimed to decrease duration of therapy, will be more accepted by the patients and be a breakthrough in treating fungal infections of the skin.

Sandwiched osmotic tablet for controlled release of metoprolol succinate

In this study novel concept of osmotically controlled drug delivery system in the form of three layered sandwiched tablet (SOT) was introduced. The tablets were prepared and optimized by design of experiment method. Metoprolol succinate, an antihypertensive agent, was selected model drug. Modified Ishikawa diagram was used to understand critical parameters that might affect the final product. Sandwiched osmotic tablets were prepared by direct compression and coated with cellulose acetate film. The process and formulation parameters were initially screened by Plackett–Burman design and later optimized by Box Behnken design. From the tablets we evaluated hardness, friability, weight variation, weight gain, coating uniformity and in vitro drug release as critical quality attributes. The amount of sodium chloride, polyethylene oxide and hydroxypropyl methylcellulose were found to influence the drug release rate from SOT as evident from Plackett–Burman design. Further these factors were optimized to get extended drug release of 80 % or more in 20 h. Optimized formulation batches (BBD8 and BBD5) showed drug release of 79.62 ± 1.19 and 82.46 ± 0.45 % respectively in 20 h with diffusion controlled zero order drug release. The check point batch prepared showed drug release of 80.86 % in 20 h. The prepared osmotically controlled sandwiched tablet showed potential to control the drug release with zero order kinetics.

Full-course inhibition of biodegradation-induced inflammation in fibrous scaffold by loading enzyme-sensitive prodrug

Biodegradation-induced inflammation in biodegradable scaffold materials is a critical problem to be addressed due to its potential inducement to tissue necrosis, granulomas, or tumor genesis. Here, a facile strategy for on-demand release of anti-inflammatory drugs and full-course inhibition of degradation-induced inflammation was demonstrated by simply loading an esterase-sensitive prodrug into a fibrous scaffold. In this study, drug release from the prodrug-loaded scaffolds showed an enzyme-triggered release process, which led to an initial moderate release of anti-inflammatory drugs and a later-stage degradation-synchronized drug release. This unique release kinetics ingeniously achieved on-demand drug therapy and efficient inhibition of inflammation throughout the biodegradation in vivo. More importantly, the prodrug-loaded scaffolds prepared with different biodegradable polymers (i.e., different biodegradation rates) all showed drug release kinetics that matched to the biodegradation rates and full-course inhibition of inflammation in vivo. Therefore, this method offered a general approach for on-demand release of anti-inflammatory drugs and efficient inhibition of inflammation throughout the biodegradation of different polymeric scaffolds. In addition, the release kinetics in our system showed potentials for “batch release” of multiple drugs in combination therapies as well as provided a feasible hint for the drug therapies of some other symptoms caused by in vivo biodegradation.

Silver nanoparticle gated, mesoporous silica coated gold nanorods (AuNR@MS@AgNPs): low premature release and multifunctional cancer theranostic platform.

Multifunctional nanoparticles integrated with an imaging module and therapeutic drugs are promising candidates for future cancer diagnosis and therapy. Mesoporous silica coated gold nanorods (AuNR@MS) have emerged as a novel multifunctional cancer theranostic platform combining the large specific surface area of mesoporous silica, which guarantees a high drug payload, and the photothermal modality of AuNRs. However, premature release and side effects of exogenous stimulus still hinder the further application of AuNR@MS. To address these issues, herein, we proposed a glutathione (GSH)-responsive multifunctional AuNR@MS nanocarrier with in situ formed silver nanoparticles (AgNPs) as the capping agent. The inner AuNR core functions as a hyperthermia agent, while the outer mesoporous silica shell exhibits the potential to allow a high drug payload, thus posing itself as an effective drug carrier. With the incorporation of targeting aptamers, the constructed nanocarriers show drug release in accordance with an intracellular GSH level with maximum drug release into tumors and minimum systemic release in the blood. Meanwhile, the photothermal effect of the AuNRs upon application to near-infrared (NIR) light led to a rapid rise in the local temperature, resulting in an enhanced cell cytotoxicity. Such a versatile theranostic system as AuNR@MS@AgNPs is expected to have a wide biomedical application and may be particularly useful for cancer therapy.

Eudragit S100 Coated Citrus Pectin Nanoparticles for Colon Targeting of 5-Fluorouracil.

In the present study, Eudragit S100 coated Citrus Pectin Nanoparticles (E-CPNs) were prepared for the colon targeting of 5-Fluorouracil (5-FU). Citrus pectin also acts as a ligand for galectin-3 receptors that are over expressed on colorectal cancer cells. Nanoparticles (CPNs and E-CPNs) were characterized for various physical parameters such as particle size, size distribution, and shape etc. In vitro drug release studies revealed selective drug release in the colonic region in the case of E-CPNs of more than 70% after 24 h. In vitro cytoxicity assay (Sulphorhodamine B assay) was performed against HT-29 cancer cells and exhibited 1.5 fold greater cytotoxicity potential of nanoparticles compared to 5-FU solution. In vivo data clearly depicted that Eudragit S100 successfully guarded nanoparticles to reach the colonic region wherein nanoparticles were taken up and showed drug release for an extended period of time. Therefore, a multifaceted strategy is introduced here in terms of receptor mediated uptake and pH-dependent release using E-CPNs for effective chemotherapy of colorectal cancer with uncompromised safety and efficacy.

Design and characterization of microsponge loaded controlled release epicutaneous gel of lornoxicam

Aim: Transdermal delivery, a successful novel approach aimed at achieving systematically active level of drug. The work involves the drug lornoxicam is a non-steroidal anti-inflammatory drug bearing analgesic, antiinflammatory, and antipyretic property. The micro sponge technology used to facilitate the controlled release of active drug into the skin in order to reduce the systematic exposure and minimize local cutaneous reactions of active drugs. The main objective of this work was to design and evaluate the gel formation of microsponge entrapped lornoxicam to increase the effectiveness of the treatment. Materials and Methods: The microsponges were prepared by quasi emulsion solvent diffusion method. The internal phase consisting eudragit RS-100 and ethyl cellulose dissolved in dichloromethane and ethyl alcohol, drug is slowly added to polymer solution with continuous stirring for 4 h, and then mixture was filtered to separate the microsponges. Microsponges was characterized by parameters like scanning electron microscopy, drug content, particle size analysis, compatibility studies using differential scanning calorimetry. Microsponge-loaded gel was characterized by physical parameters of gel, measurement of PH, viscosity study, Drug content study, in-vitro release studies using first order kinetics, Higuchi Model, Peppas release Model. Results: The different kinetics models showed that the release data followed Higuchi matrix and the release mechanism from microsponges was diffusion. Conclusion: From the results, it can be concluded that LMF3 formulation shows drug release in a controlled manner.

Evaluation of Binding Property ofRemusatia vivipara(Roxb) Mucilage in Tablet Formulation

Remusatia vivipara is a common herbaceous belongs to the family of Araceae. Tubers of plant contain mucilage hence attempt to evaluate the tubers for suitability as tablet binder is considered and the present investigation repots the isolation of mucilage of Remusatia vivipara tubers. The DSC and FTIR thermograms of drug and mucilage indicated no chemical interaction. Phytochemical and Physiochemical characteristics of mucilage were studied which confirmed the mucilage nature. The mucilage was evaluated for its granulating and binding properties in compressed tablet using Metformin HCl as model drug. The granules prepared by mucilage with different concentration such as 1%, 3%, 5% and 10% were compared with starch paste, which was used as standard binder. The tablets had good physiochemical properties and the drug release was more than 95% within 24hr. It was observed that decreasing the concentration of mucilage increases hardness and the disintegration time. The tablet prepared using 1% and 3% shows drug release rate in sustained manner and that of standard binder 10% starch paste used for comparison. Remusatia vivipara mucilage could be used as a good binding agent at very low concentrations. This can be used for sustaining the drug release from tablets, since the prepared tablets produced a sticky film of hydration on the surface, which ultimately reduces drug release rate and hence it can be evaluated for its efficacy to sustain the drug release.

Development of Mucoadhesive Nanoparticulate System of Ebastine for Nasal Drug Delivery

Purpose: To prepare and evaluate mucoadhesive nanoparticulate system of ebastine for nasal drug delivery.Methods: The nanoparticles were prepared by ionic gelation method using drug-chitosan weight ratios 1:1, 1:2 and 1:3, and incorporating 0.5 or 0.7 % w/v sodium tripolyphosphate (STPP) and poloxamer 407. The mucoadhesive nanoparticles were characterized by scanning electron microscope (SEM), transmission electron microscope (TEM), differential scanning colorimetry (DSC) and Fourier transform infrared spectroscopy (FTIR) and evaluated for drug loading, entrapment efficiency, in vitro mucoadhesion, in vitro drug release and ex-vivo permeation.Results: FTIR and DSC studies indicate that no chemical interaction occurred between the drug and polymer. Nanoparticle size ranged from 169 to 500 nm. Drug loading and entrapment efficiency increased with increase in chitosan concentration and decreased with increase in poloxamer 407 concentration. The highest drug loading obtained for the nanoparticles was 19.5 %. With increase in polymer (chitosan) concentration (1:1 to 1:3), production yield was unchanged (73.2 to 74.4 % (F6)). Mucoadhesion increased with increase in the concentration of chitosan. In vitro drug release from all the formulations was biphasic, being characterized by a slight ‘burst’ followed by slow release. At the end of 8 h F6 (1:3) showed drug release of only 86.9 %, indicating sustained release. Ex-vivo permeation of pure ebastine was more rapid than from F6, thus indicating the capability of chitosan to control drug permeation rate through sheep nasal mucosa.Conclusion: The results indicate that a mucoadhesive nanoparticulate system can be used effectively for the nasal delivery of the antihistamine, ebastine.Keywords: Chitosan, Ebastine, Mucoadhesive, Nanoparticles, Ionotropic gelation, Permeation, Drug release, Poloxamer

Design, development, in vitro and in vivo evaluation of multicomponent tablet formulation for enteral delivery of atorvastatin calcium and felodipine

Frequent occurrence, higher morbidity and mortality rate of atherosclerosis associated hypertension in elderly people shambles health care system worldwide. So the present study was deliberated to formulate and appraise rational combination, containing immediate release portion of atorvastatin calcium (ATR) and sustained release (SR) portion of felodipine (FEL) in bilayered multicomponent tablet formulation for elderly people. A 32 factorial design was used to prepare atorvastatin calcium and felodipine tablets separately. For each drug total nine batches (A1–A9 for ATR; F1–F9 for FEL) were prepared. The amount of sodium starch glycollate (X1) and lactose (X2) were used as independent variables for atorvastatin calcium and hydroxypropyl methyl cellulose 50 cps (X1) and talc (X2) for felodipine tablets. Talc being hydrophobic diluents has been tried as release retardant. On the basis of flowability, compressibility, compactibility, tensile strength and drug release, the both layers of formulation were optimized, and subsequently, bilayered multicomponent tablet formulation was prepared and evaluated. The optimized tablet formulations of atorvastatin calcium (Batch A3) released 76 % of drug after 30 min, while (Batch F8) of felodipine showed drug release up to 79 % after 10 h and followed peppas release pattern (r2 = 0.9862). The similar release pattern was noticed in the bilayered tablet formulation of atorvastatin calcium and felodipine meeting the USP requirements. Hence, it can be concluded that, the aforesaid bilayered formulation can meet the needs of those elderly people, who suffer from mild hypertension and hyperlipidemia.

Implications of formulation design on lipid-based nanostructured carrier system for drug delivery to brain

Context & Objective: The aim of present investigation was to formulate and develop lipid-based nanostructured carriers (NLCs) containing Idebenone (IDE) for delivery to brain. Attempts have been made to evaluate IDE NLCs for its pharmacokinetic and pharmacodynamic profile through the objective of enhancement in bioavailability and effectivity of drug.Methods: Nanoprecipitation technique was used for development of drug loaded NLCs. The components solid lipid Precirol ATO 5, oil Miglyol 840, surfactants Tween 80 and Labrasol have been screened out for formulation development by consideration of preformulation parameters including solubility, Required Hydrophilic lipophilic balance (HLB) of lipids and stability study. Developed IDE NLCs were subjected for particle size, zeta potential, entrapment efficiency (%EE), crystallographic investigation, transmission electron microscopy, in vitro drug release, pharmacokinetics, in vivo and stability study.Results: Formulation under investigation has particle size 174.1 ± 2.6 nm, zeta potential −18.65 ± 1.13 mV and% EE 90.68 ± 2.90. Crystallographic studies exemplified for partial amorphization of IDE by molecularly dispersion within lipid crust. IDE NLCs showed drug release 93.56 ± 0.39% at end of 24 h by following Higuchi model which necessitates for appropriate drug delivery with enhancement in bioavailability of drug by 4.6-fold in plasma and 2.8-fold in brain over plain drug loaded aqueous dispersions. In vivo studies revealed that effect of drug was enhanced by prepared lipid nanocarriers.Conclusions: IDE lipid-based nanostructured carriers could have potential for efficient drug delivery to brain with enhancement in bioavailability of drug over the conventional formulations.

Composite wound dressing for drug release

Present study is focused on the preparation of two layers composite wound dressing for drug release. The outer layer is made of hydrogel which contains of drug and the core layer is made of fabric. The two layers structure of composite dressing is formed by grafting of polyacrylamide-co-acrylic acid hydrogel on cotton fabric using ammonium per sulphate (APS) as chemical initiator and polyethylene glycol (PEG) as crosslinker. The major factors affecting graft copolymerization of hydrogel on cotton fabric are optimized by varying concentration of monomers & initiator, reaction temperature and addition time of crosslinker. Maximum grafting of hydrogel is obtained at 5 % (w/v) APS and 15 % acrylamide/acrylic acid (1:1 w/w ratio) concentration. The FTIR spectra of composite dressing shows characteristics peak of acrylic acid and acrylamide. The composite wound dressing material is loaded with model drug bovine serum albumin (BSA) and drug release behaviour is studied at different pH. The dressing shows drug release in different pH with maximum release of drug in acidic medium.

RIFAMPICIN LOADED SPRAY-DRIED OLIBANUM GUM RESIN PULMOSPHERES FOR LUNG DELIVERY

Pulmospheres of Rifampicin were prepared successfully with cyclodextrin using olibanum gum resin as a rate controlling biodegradable natural polymer by novel spray drying technique. Hydroxypropyl-β-cyclodextrin was used as solubilising agent to enhance the solubility and permeation of poorly soluble rifampicin. The physcochemical characteristics of  rifampicin loaded pulmospheres were evaluated for mean particle size, thermal behaviour and surface morphology. The mean particle size for optimized formulation F1 was found to be 3.5 µm and spray-dried pure rifampicin also showed same value. Scanning Electron Microphotographs of pure drug has shown a typical and regular size indicated crystalline nature, whereas, spray dried pure drug and formulation F1 have shown spherical particles with porous surface indicated the conversion of crystalline drug into amorphous form. Rifampicin loaded spray-dried pulmospheres using olibanum gum resin showed drug release up to 72 hours. The release of rifampicin was greater in simulated physiological fluid of pH 7.4 which was 94 % as compared to simulated lung fluid of pH 5.2 at the end of 72 hours. Rifampicin loaded spray-dried microspheres were proposed for pulmonary drug delivery.  Keywords: Rifampicin, Lung targeting, Olibanum gum resin, Spray-drying, Pulmospheres

Formulation and Evaluation of Metaprolol tartarate Non-effervescent Gastric Floating tablets

Plan: The objective of this study was to develop Gastric floating drug delivery system containing Metoprolol and having a bulk density lower than that of gastric fluid remaining buoyant on the stomach contents. Preface: Metaprolol tartarate is having short to moderate half life 3-7 hrs, low bioavailability hence it is worth able to formulate Metaprolol in floating drug delivery. The GRDDS can improve the controlled delivery of the drugs which exhibit an absorption window by continuously releasing the drug for a prolonged period before it reaches its absorption site, thus ensuring its optimal bioavailability Methodology: Percentage drug content in all floating tablet formulations was found to be 95.85% to 103.33% which was within Pharmacopoeial limit. In- vitro drug release profile from all formulations (F1-F10) showed sustained release of Metoprolol Tartarate over a period of 10 hours. Outcome: Among all the formulation, F3 showed drug release up to 94.71% at the end of 10 hours. The mechanism of the drug release from F3 was anomalous transport, first order release kinetics. Stability studies on optimized batch showed no significant effect on physical properties, drug content, floating behavior and drug release.