Improved pharmaceutical properties of surface modified bioactive plumbagin crystals

Bothiraja, C.; Pawar, Atmaram; Mali, Ashwin J.; Shaikh, Karimunnisa S.

doi:10.1504/ijsurfse.2013.053708

Cited by 14 publications

(9 citation statements)

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“…Animal studies suggested that orally administered PLB produces only 39% of bioavailability owing to its limited biopharmaceutical properties such as high lipophilicity, insolubility in water, short biological half-life and low melting point [24]. Being a quinine moiety is reported to be highly toxic and acts as spindle poison by inhibiting cell mitosis at low concentrations and by exhibiting radiomimetic and cytotoxic effects at higher concentrations.…”

Section: Plb Delivery Systemsmentioning

confidence: 99%

“…Bothiraja et al prepared surface modified PLB crystals by cold recrystallization technique using a variety of polar and nonpolar solvents [49]. Platy crystals, the most significant forms, obtained from cyclohexane possessed small size (62.93 ± 3.74 lm), higher bulk density (0.108 ± 0.014 g/ml) and lower enthalpy of fusion (DH 62.62 ± 3.67 J/g).…”

Section: Miscellaneousmentioning

confidence: 99%

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Current development in novel drug delivery systems of bioactive molecule plumbagin

Rajalakshmi¹,

Vyawahare²,

Pawar

et al. 2018

Artificial Cells, Nanomedicine, and Biotechnology

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Plumbagin (PLB), a member of the quinine family, mainly found in the plant Plumbago zeylanica Linn., potentially exhibit anticancer, anti-inflammatory, anti-oxidant, antifungal, neuroprotective, hypolipidemic and antibacterial activities. However, it has been well known that the application of PLB was limited owing to its water insolubility, instability and poor bioavailability. For decades, many attempts have been made to compensate for these disadvantages with the development of improved delivery platforms as the feasible approaches. This review aims to describe the various studies supporting the biopharmaceutical aspects of PLB. In addition, it includes a section devoted to discussing the challenges associated with the drug and strategies to improve the properties of PLB such as solubility, stability and bioavailability. Also, this paper summarizes the recent works on the design and development of novel delivery systems of PLB such as liposomes, niosomes, microsphares, nanoparticles, micelles, complexization, metal nanoparticles, crystals modification, etc., with the goal of harnessing the true difficulties of this multifunctional agent in the clinical arena.

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Section: Plb Delivery Systemsmentioning

confidence: 99%

Section: Miscellaneousmentioning

confidence: 99%

Current development in novel drug delivery systems of bioactive molecule plumbagin

Rajalakshmi¹,

Vyawahare²,

Pawar

et al. 2018

Artificial Cells, Nanomedicine, and Biotechnology

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“…The researchers concluded that surface modification led to enhanced efficacy of plumbagin. This approach is capable of improving the bioavailability and clinical efficacy of other poorly water soluble phytomedicines 106 .…”

Section: Guggulsterone [4 17(20)-pregnadiene-3 16-dione]mentioning

confidence: 99%

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2013

IJPSR

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Arthritis is still a challenge for medical research. Pharmaceutical research has resulted in several new approaches for treatment/management of arthritis including drugs like the biologic disease modifying anti-rheumatic drugs (DMARDs). Several disadvantages like serious side effects, high costs and requirement of parenteral administration still invite more research in this area to provide a convenient, affordable therapy with lesser or no side effects. Traditionally used herbal medicines, due to their anti-inflammatory and immunomodulatory properties, have potential to be a therapy of choice for arthritis patients and are now extensively being studied. Although a number of these medicines are being used traditionally for their therapeutic activity, development of their novel drug delivery systems was not attractive to the scientists due to insufficient knowledge about their exact mechanism of action and difficulties in processing, standardising, extracting and identification of active constituents. Current research demonstrates that the effectiveness and bioavailability of herbal actives can be improved by understanding of exact mechanism of action and by formulating them into novel technologies like liposomes, phytosomes and transdermal drug delivery. The present review focuses on herbal medicines for arthritis along with various strategies adopted by scientists so as to improve the bioavailability, stability and to reduce the side effects of these medicines so as to provide consistently effective alternative medication for arthritis. The strategies include understanding mechanisms of their action, enhancing solubilities of poorly soluble actives and developing novel drug delivery systems of these herbal medicines.

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“…Poor aqueous solubility as well high intra-and inter subject inconsistency are considered to be main barricades for poor oral bioavailability. A number of formulation approaches, such as solid dispersions, salt formation, micronization, cyclodextrin complexation, micellar solutions, nanoparticulates to improve the oral absorption of drugs 1,2 . Hydrotropy is one of the recognized techniques available to enhance the aqueous solubility of a drug.…”

Section: Introductionmentioning

confidence: 99%

Novel Application of Mixed Hydrotropic Solubilization Technique in the Formulation and Evaluation of Solid Dispersion of Flupirtine Maleate

Yadav

Shukla

Upmanyu

et al. 2018

J. Drug Delivery Ther.

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Flupirtine is an amino pyridine derivative that functions as a centrally acting non-opioid, non-steroidal analgesic. It is a selective neuronal potassium channel opener that also has NMDA receptor antagonist properties. Its muscle relaxant properties make it popular for back pain and other orthopedics uses. In the present investigation, recently developed mixed hydrotropic solid dispersion technology precludes the use of organic solvent and also decreases the individual concentration of hydrotropic agents, simultaneously decreasing their toxic potential. Mixed-hydrotropic solubilisation technique is the experience to increase the solubility of poorly water soluble drugs in the aqueous solution containing blends of hydrotropic agents, which may give synergistic enhancement effect on solubility of poorly water-soluble drugs and to reduce concentrations of each individual hydrotropic agent to minimize their toxic effects due to high concentration of hydrotropic agents. The Flupirtine loaded solid dispersion was prepared by a solvent evaporation technique using sodium benzoate and a niacinamide hydrotropic mixture. The prepared solid dispersions were valuated regarding their solubility, mean particle size, in-vitro drug release. The prepared solid dispersions were found very stable (chemically). The superior dissolution rate due to its reduced particle size may have contributed to the increased oral bioavailability. This study demonstrated that mixed-solvency may be an alternative approach for poorly soluble drugs to improve their solubility and oral bioavailability. Novel application of mixed hydrotropic solubilization technique in the formulation and evaluation of solid dispersion of flupirtine maleate, Journal of Drug Delivery and Therapeutics. 2018; 8(5):481-488 DOI: http://dx.

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Improved pharmaceutical properties of surface modified bioactive plumbagin crystals

Cited by 14 publications

References 0 publications

Current development in novel drug delivery systems of bioactive molecule plumbagin

Current development in novel drug delivery systems of bioactive molecule plumbagin

Untitled

Novel Application of Mixed Hydrotropic Solubilization Technique in the Formulation and Evaluation of Solid Dispersion of Flupirtine Maleate

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