FABRICATION AND CHARACTERIZATION OF RALOXIFENE LOADED SOLID-LIPID NANOPARTICLES

Objective:  The poor water solubility of the drug presents a great challenge for the formulation development and results in low oral bioavailability. The oral bioavailability of Raloxifene HCl (RLX) is very low (<2%) in humans due to its poor solubility. The objective of the present study was to develop RLX loaded solid-liquid nanoparticles for effective drug delivery. Methods: Compritol 888 ATO-based RLX-loaded solid lipid nanoparticles (SLNs) were formulated using the oil in water microemulsion method. Drug-excipients compatibility was confirmed through Fourier transform infrared spectroscopy, Differential scanning calorimetry methods. The SLN was characterized for particle size, surface morphology, entrapment efficiency. Results: A total of seventeen formulations (SLN1-SLN17) were developed as per the 3 levels 3 factor Box–Behnken design. The model used for the analysis was statistically analyzed using ANOVA and the goodness of fit was evaluated using diagnostic plots. As per the response-surface plots, the amount of lipid, poloxamer 407, and ultrasonication time have a significant effect on the particle size and entrapment efficiency (%EE). The developed RLX-loaded SLNs have the size and %EE in the range of 165.63±2.62 nm to 315.33±4.87 nm and 75.21±2.32% to 95.32±2.11%. The TEM analysis showed that the developed RLX-loaded SLNs were almost spherical and has a small size range. Conclusion: The high biocompatibility, biodegradability, ability to protect drugs in GIT, and sustained release properties make SLNs an ideal candidate to resolve poor oral bioavailability challenges

AN UPDATED REVIEW ON TRANSFERSOMES: A NOVEL VESICULAR SYSTEM FOR TRANSDERMAL DRUG DELIVERY

Transdermal route is an interesting option in this respect because a transdermal route is convenient and safe, avoid first pass metabolism, predictable and extended duration of activity, minimizing undesirable side effects, utility of short half-life drugs, improving physiological and pharmacological responses, avoiding the fluctuation in drug levels and inter and intra-patient variations. However it has got its own limitations its inability to transport large molecules, inability to overcome the barrier properties of stratum corneum and many more. Formulating the drug in a transfersome is one such approach to solve these problems. Transfersome, is an ultradeformable vesicle, elastic in nature which can squeeze itself through a pore which is many times smaller than its size owing to its elasticity. Peer Review History: Received 29 August 2017;   Revised 5 September; Accepted 9 September, Available online 15 September 2017 Academic Editor: Dr. DANIYAN Oluwatoyin Michael, Obafemi Awolowo University, ILE-IFE, Nigeria, [email protected] UJPR follows the most transparent and toughest ‘Advanced OPEN peer review’ system. The identity of the authors and, reviewers will be known to each other. This transparent process will help to eradicate any possible malicious/purposeful interference by any person (publishing staff, reviewer, editor, author, etc) during peer review. As a result of this unique system, all reviewers will get their due recognition and respect, once their names are published in the papers. We expect that, by publishing peer review reports with published papers, will be helpful to many authors for drafting their article according to the specifications. Auhors will remove any error of their article and they will improve their article(s) according to the previous reports displayed with published article(s). The main purpose of it is ‘to improve the quality of a candidate manuscript’. Our reviewers check the ‘strength and weakness of a manuscript honestly’. There will increase in the perfection, and transparency. Received file:        Reviewer's Comments: Average Peer review marks at initial stage: 4.5/10 Average Peer review marks at publication stage: 7.0/10 Reviewer(s) detail: Dr. Omonkhelin J Owolabi, University of Benin, Nigeria, [email protected] Dr. Taiwo O Elufioye, University of Ibadan, Nigeria, [email protected] Similar Articles: INVESTIGATION OF PRONIOSOMES GEL AS A PROMISING CARRIER FOR TRANSDERMAL DELIVERY OF GLIMEPIRID

Development and evaluation of floating microspheres of curcumin in alloxan-induced diabetic rats

Purpose: To prepare and evaluate floating microspheres of curcumin for prolonged gastric residence and to study their effect on alloxan-induced diabetic rats.Methods: Floating microsphere were prepared by emulsion-solvent diffusion method, using hydroxylpropyl methylcellulose, chitosan and Eudragit S 100 polymer in varying proportions. Ethanol/dichloromethane blend was used as solvent in a ratio of 1:1. The floating microspheres were evaluated for flow properties, particle size, incorporation efficiency, as well as in-vitro floatability and drug release. The anti-diabetic activity of the floating microspheres of batch FM4 was performed on alloxaninduced diabetic rats.Result: The floating microspheres had particle size, buoyancy, drug entrapment efficiency and yield in the ranges of 255.32 - 365.65 μm, 75.58 - 89.59, 72.6 - 83.5, and 60.46 - 80.02 %, respectively. Maximum drug release after 24 h was 82.62 % for formulation FM4 and 73.879, 58.613 and 46.106 % for formulations FM1, FM2, and FM3 respectively. In-vivo data obtained over a 120-h period indicate that curcumin floating microspheres from batch FM4 showed the better glycemic control than control and a commercial brand of the drug.Conclusion: The developed floating curcumin delivery system seems economical and effective in diabetes management in rats, and enhances the bioavailability of the drug.Keywords: Gastro-retentive, Sustained release, Bioavailability, Curcumin, Floating microspheres, Diabete

Enhancing Oral Bioavailability of Poorly Water Soluble Drugs through Solid Lipid Nanoparticles: Recent Advancements

To date, the oral route is considered as a proffered route for drug delivery having high patient compliance. However, the therapeutic efficacy of the drug given through the oral route is hampered by its low solubility, low bioavailability, and stability issues in the harsh gastric environment. Solid lipid nanoparticles (SLNs) have emerged as a potential system that can overcome the oral bioavailability issues associated with poorly water-soluble drugs. The SLNs have both properties of lipid emulsion and polymeric nanoparticles and thus offer various benefits, such as high biocompatibility, biodegradability, protect the drug from degradation, improved drug stability in gastrointestinal tract, controlled drug release, avoid organic solvents, and ease of manufacturing. This review discussed the recent advancements in SLNs with regards to the oral bioavailability of poorly water-soluble drugs. The key components and methods of preparation of SLNs were also discussed. To conclude, studies performed to date have shown promising results with SLNs in enhancing the oral bioavailability of poorly water-soluble drugs with a high degree of biocompatibility

Pinus roxburghii stand dynamics at a heavily impacted site in Nepal: Research through an educational fieldweek

The fieldweek associated with the 4th Asian Dendrochronological Association Conference was an excellent opportunity for education, networking, and research. The participants and group leaders worked together for five days in an area that was new to some of the group leaders and new to some of the participants which enabled us to learn about forest ecology around Kathmandu and Nagarkot, Nepal. The fieldweek was an excellent networking opportunity and the group leaders and participants bonded which strengthened international research in dendrochronology and continues to foster new research collaborations. All of the group leaders and participants had the opportunity to learn about tree-ring formation in Pinus roxburghii at 1500 masl elevation, to explore its wood anatomy, and to examine specific research questions in our field area. In the end we developed a better understanding of the stand-age structure of a stand of trees in Nagarkot, explored the erosion history from exposed roots, and investigated tree health issues on closely related sites. We found that P. roxburghii poses some dating issues with false and micro rings at this elevation, but we were still able to develop a tree-ring chronology from this species and make preliminary assessments of stand dynamics and health

Pinus roxburghii stand dynamics at a heavily impacted site in Nepal: Research through an educational fieldweek

The fieldweek associated with the 4th Asian Dendrochronological Association Conference was an excellent opportunity for education, networking, and research. The participants and group leaders worked together for five days in an area that was new to some of the group leaders and new to some of the participants which enabled us to learn about forest ecology around Kathmandu and Nagarkot, Nepal. The fieldweek was an excellent networking opportunity and the group leaders and participants bonded which strengthened international research in dendrochronology and continues to foster new research collaborations. All of the group leaders and participants had the opportunity to learn about tree-ring formation in Pinus roxburghii at 1500 masl elevation, to explore its wood anatomy, and to examine specific research questions in our field area. In the end we developed a better understanding of the stand-age structure of a stand of trees in Nagarkot, explored the erosion history from exposed roots, and investigated tree health issues on closely related sites. We found that P. roxburghii poses some dating issues with false and micro rings at this elevation, but we were still able to develop a tree-ring chronology from this species and make preliminary assessments of stand dynamics and health. (C) 2016 Elsevier GmbH. All rights reserved