18 research outputs found

    Sustained Release Solid Dispersions of Pentoxyfylline: Formulation and Optimization

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    Objective: The purpose of the study is to formulate and optimize sustained release solid dispersions of pentoxyfylline using a combination of eudragit polymers and ethyl cellulose. Methods: Solid dispersions were formulated by solvent evaporation method.Preliminary batches were formulated using various drug to polymer ratio; with eudragit S100 and L100 (1:1 to 1:5 ratio), and with ethyl cellulose(1:1 to 1:3 ratio) and evaluated for solubility analysis. Based on results of preliminary batches, Box Behnken design was further applied and three factors (X1- concentration of Eudragit S100, X2- concentration of Eudragit L100, X3- concentration of Ethyl Cellulose) were selected with three levels (+1, 0, -1). Multiple linear regression was applied to generate polynomial equations and statistical evaluation. Prepared solid dispersions were investigated for sustained release properties via in vitro dissolution studies. Fourier transform infrared spectroscopic analysis (FTIR), X-ray diffraction analysis (X-RD), Differential scanning calorimetry (DSC) studies were carried out to evaluate drug polymer interactions. Scanning Electron Microscopy (SEM) analysis of optimized solid dispersion was carried out to evaluate surface morphology of the particles. Results: Batch F5 showed maximum sustained release (65.46% in 24 h) characteristics out of all solid dispersions. DSC studies indicated drug integrity when mixed with the polymeric carriers. FTIR and X-RD studies also ruled out any drug polymer interaction. A change in crystalline habit was observed in solid dispersion particles (F5 batch) as seen in SEM micrographs. Polynomial mathematical model generated using multiple regression analysis was found to be statistically significant (p<0.05). Conclusion: Release retarding effect was found to be dependent on polymer concentration. Therefore, an optimized combination may lead to better sustaining effect

    An Update on Some Recent Solubility Enhancers as Pharmaceutical Excipients

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    At present the pharmaceutical academia and industries are focusing on the use of natural materials and resources for development of pharmaceutical product. Due to advances in drug delivery technology, currently, excipients are included in novel dosage forms to fulfill specific functions. Various natural polymers are widely being studied as a potential carrier material for site specific drug delivery because of its non-toxic and biocompatible in nature. Natural polymers (polysaccharides) have been investigated for drug delivery applications as well as in biomedical fields. Modified polymer or synthetic polymers have found its application as a support material for cell culture, tissue engineering and gene delivery. Recent trends towards use of natural products or plant based products demand the replacement of synthetic additives with natural ones. These natural materials have many advantages over synthetic ones as they are biodegradable, chemically inert, less expensive, nontoxic and widely available. This review provides an overview of the different modified polymer derivatives and their applications with special consideration being put on biomedical engineering and controlled drug delivery

    Microneedle Mediated Vaccine Delivery: A Comprehensive Review

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    Microneedles can be representative for paradigm shift of drug delivery from patient non-compliant parenteral injections to patient compliant drug delivery system, which can be utilized for administration of vaccines particularly along with macromolecular/micromolecular drugs. The concept of microneedles came into existence many decades ago but the use of microneedles to achieve efficient delivery of drugs into the skin became subject of research from mid of 1990’s. Various types of microneedles were utilized to enhance delivery of drugs and vaccines including solid microneedles for pre-treatment of skin to enhance drug permeability, dissolvable polymeric microneedles encapsulating drugs, microneedles coated with drugs and hollow microneedles for infusion of drugs through the skin. Microneedles have shown promisingdelivery of vaccines through skin in literature. But the successful utilization of this system for vaccine drug delivery mainly depends on design of device to facilitate microneedle infusion, vaccine stability and storage in system, recovery of skin on removal of microneedle and improved patient compliance. This article reviews the conventional and advanced methods of vaccine drug deliver, microneedles for drug delivery, types of microneedles, advantages of microneedles and potential of microneedles for vaccine drug delivery

    Dissolution Enhancement of Domperidone Fast Disintegrating Tablet Using Modified Locust Bean Gum by Solid Dispersion Technique

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    Enhancement of dissolution characteristics of poorly soluble drug Domperidone by solid dispersion technique using modified locust bean gum (MLBG) and further conversion into tablet dosage form with fast dissolving characteristics is being explored in current study. Solid dispersions (SD) were prepared by solvent evaporation technique. F1, F3, F5 and F7 batches of SD (1:1, 1:3, 1:5 and 1:7 ratio of drug to MLBG) were prepared. Maximum solubility was observed in 1:3 ratio (F3 batch) in comparison to pure drug. Fourier Transform Infrared spectroscopy studies revealed no interaction of drug to polymer MLBG. Transition from crystalline to amorphous state of drug was analyzed by X-RD studies. SEM studies revealed change in surface characteristics of drug in solid dispersions. In vitro release studies revealed maximum dissolution in F3 (93% in 30 min). Further solid dispersion batches F3 was compressed into tablets including other excipients and crosspovidone as superdisintegrant. The in vitro release from tablet batch revealed better dissolution characteristics (95% in 30 min) in comparison to marketed tablet (50% in 60 min). Therefore, MLBG solid dispersion tablets of domperidone can be a convenient dosage form with enhanced dissolution characteristics

    Modified Excipients in Novel Drug Delivery: Need of the Day

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    Drug products not only contain “actives” that confer the intended therapeutic benefits such as pain relief or act on particular part of the body, but contain other materials that are also “functional” with respect to the drug product. These are known as excipients and specific functionality which they confer to a particular product is independentupon the process used to add the excipient to the formulation and its exact location within the final dosage form. Introduction of novel drug delivery systems and new drugmoieties lead to the need for new excipients with varied characteristics. Development of new excipient entities and their evaluation is a costly procedure; modificationof existing excipients is very easy, more economical and less time consuming. The development of excipients that are capable of fulfilling multifunctional roles such asenhancing drug bioavailability and drug stability as well as controlling the release of the drug according to the therapeutic needs is one of the most important prerequisitesfor further progress in the design of novel drug delivery systems. The main focus of this article is on synthetic novel excipients that perform multiple functions inpharmaceutical formulations

    Starch-silicon dioxide coprecipitate as superdisintegrant: formulation and evaluation of fast disintegrating tablets

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    The objective of the present investigation is to synthesize and characterize starch-silica coprecipitate and evaluate as tablet superdisintegrant. The starch-silica coprecipitate was synthesized by coprecipitation of silica on the surface of starch particles as reported by Rashid et al. The coprecipitate was characterized in terms of compressibility characteristics, Differential Scanning Calorimetry (DSC) and Fourier Transformed Infra Red Spectroscopy (FTIR). Fast dissolving tablets were then formulated by direct compression method using the different concentration of coprecipitate, crosscarmellose sodium (CCS) and crosspovidone (CP) as superdisintegrant. The tablets were evaluated for the disintegration time, hardness, friability, tensile strength, weight variation and in vitro release studies. The starch-silica coprecipitate showed better disintegration and compressibility characteristics as compared to the known superdisintegrants. FTIR indicated the absence of any chemical reaction between the two species (starch and silica) during the process of coprecipitation. DSC studies showed there is no interaction between the drug and coprecipitate. Hausner’s ratio & Carr’s index value of (1.17 and 14.7 respectively) of coprecipitate suggested excellent flowability. The coprecipitate was found to be effective at all the concentrations tested in the fast dissolving tablet formulation. Disintegration time (DT) of less than 30 seconds was observed in case of coprecipitate whereas higher DT values was observed with CCS and CP as superdisintegrants. Starch-silica coprecipitate can be utilized as a superdisintegrant in the pharmaceutical applications owing to better compressibility and release characteristics

    Development and Optimization of Fast Dissolving Tablets of Losartan Potassium Using Natural Gum Mucilage

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    Current research work involves preparation of fast dissolving tablets of Losartan Potassium by direct compression method using different concentrations of Plantago ovata and Lepidium sativum mucilage as natural superdisintegrants. A two factor three level (32) factorial design is being used to optimize the formulation. Nine formulation batches (A1-A9) were prepared by taking two factors as independent variables (X1- amount of Plantago ovata mucilage and X2- amount of Lepidium sativum mucilage)were taken with three levels (+1, 0, -1). All the active blends were evaluated for precompression parameters (angle of repose, bulk density, carr’s index, hausner’s ratio) and formulated tablets were evaluated for post compression parameters (hardness, friability, weight variation, wetting time, disintegration time, water absorption ratio). In vitro drug release studies were carried out using USP II dissolution apparatus for 30 min. The software Design Expert (8.0.7.1) was used for generating experimental design, modeling the response surface and calculating the statistical evaluation. Tablet parametric tests of formulation batches (A1-A9) of FDT were found within prescribed limits.DT was observed in the range from 12±2 to 58.7±2.52 sec and WT from 10.3±1.52 to 49.7±5.13 sec for formulation batches (A1-A9). More than 87% drug release was observed in all formulation batches (A1-A9) within 15 minutes. Polynomial mathematical models, generated for various response variables using multiple linear regression analysis, were found to be statistically significant (P < 0.05). Formulation A7 was selected by the design expert software which exhibited DT (22.15sec), WT (17.31sec) and in vitrodrug release (100%) within 15 minutes

    Potential benefits of phytochemicals for treatment of hyperpigmentation

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    UV radiation (UV) is considered as a complete carcinogen as it is both a mutagen and a non-specific damaging agent. It is the most important risk factor for skin cancer and many other skin disorders like Hyperpigmentation. There is a need of long-term topical skin care treatments (both cosmetic and cosmeceutical) to address problems associated with hyperpigmentation. Synthetic depigmenting agents, such as hydroquinone, mequinol, although highly effective, can raise several safety concerns (for example, ochronosis, cataract, impaired wound healing, desquamation, and other local or systemic side effects) with long-term exposure. The benefits of phytochemicals and natural extracts offer opportunities to develop new formulations to treat pigmentation problems. Cosmeceuticals are topical cosmetic-pharmaceutical preparations containing active ingredients which improve the appearance of skin. Among cosmeceuticals, the phytochemicals have been known to have a multitude of cellular actions for various dermatological diseases. Plant-derived compounds and their effectiveness in the treatment of hyperpigmentation disorders (Melasma) are discussed. Keywords: UV radiation, Hyperpigmentation, Phytochemicals, Cosmeceutical

    Improved antibacterial activity of topical gel-based on nanosponge carrier of cinnamon oil

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    Introduction: Cinnamon essential oil (CEO) is a volatile oil, obtained from Cinnamomum zeylanicum has become one of the most important natural oil due to its antimicrobial activity. CEO suffers from various limitations such as instability and skin irritation. This problem has been overcome by formulating CEO-loaded nanosponges incorporated in carbopol gel with increased antimicrobial property and reduced skin irritation. Methods: The nanosponges were fabricated by solvent emulsion diffusion method and evaluated for Fourier transform infrared spectroscopy (FTIR) studies, particle size, field emission scanning electron microscopy studies (FE-SEM), in vitro dissolution studies, in vitro antibacterial studies, using agar diffusion method, in vivo antibacterial activity and skin irritation studies and stability studies. Results: Nanosponge NS1 batch was found to be in the nanosize range. FTIR studies confirmed the absence of drug-polymer interaction. NS1 confirmed a porous structure with a uniform spherical shape using FE-SEM studies. In vitro dissolution studies of optimized NS1 revealed 80% drug release in 5 h whereas, incorporating the formulation into carbopol gel showed 100% release in 5h from G1 formulation. In vitro antibacterial study of the nanosponge (NS1 and NS3) showed remarkable antibacterial activity as seen from the zone of inhibition and gel formulation G1 also showed the highest zone of inhibition with 50±1.2 mm. NS1 and G1 were stable for 2 months under accelerated conditions and 3 months under room temperature conditions. Furthermore, the in vivo and skin irritation studies were performed with selected formulation against Staphylococcus aureus, where the results confirmed the significant antimicrobial activity with no skin irritation. Conclusion: Nanosponge carriers can be more therapeutically effective for essential oils which can further be incorporated into topical gels for convenient application

    Dissolution Improvement of Atorvastatin Calcium using Modified Locust Bean Gum by the Solid Dispersion Technique

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    The present research was aimed at the enhancement of the dissolution rate of atorvastatin calcium by the solid dispersion technique using modified locust bean gum. Solid dispersions (SD) using modified locust bean gum were prepared by the modified solvent evaporation method. Other mixtures were also prepared by physical mixing, co-grinding, and the kneading method. The locust bean gum was subjected to heat for modification. The prepared solid dispersions and other mixtures were evaluated for equilibrium solubility studies, content uniformity, FTIR, DSC, XRD, in vitro drug release, and in vivo pharmacodynamic studies. The equilibrium solubility was enhanced in the solid dispersions (in a drug:polymer ratio of 1:6) and other mixtures such as the co-grinding mixture (CGM) and kneading mixture (KM). Maximum dissolution rate was observed in the solid dispersion batch SD3 (i.e. 50% within 15 min) with maximum drug release after 2 h (80%) out of all solid dispersions. The co-grinding mixture also exhibited a significant enhancement in the dissolution rate among the other mixtures. FTIR studies revealed the absence of drug-polymer interaction in the solid dispersions. Minor shifts in the endothermic peaks of the DSC thermograms of SD3 and CGM indicated slight changes in drug crystallinity. XRD studies further confirmed the results of DSC and FTIR. Topological changes were observed in SEM images of SD3 and CGM. In vivo pharmacodynamic studies indicated an improved efficacy of the optimized batch SD3 as compared to the pure drug at a dose of 3 mg/kg/day. Modified locust bean gum can be a promising carrier for solubility enhancement of poorly water-soluble drugs. The lower viscosity and wetting ability of MLBG, reduction in particle size, and decreased crystallinity of the drug are responsible for the dissolution enhancement of atorvastatin. The co-grinding mixture can be a good alternative to solid dispersions prepared by modified solvent evaporation due to its ease of preparation and significant improvement in dissolution characteristics
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