Development of Microemulsion Based Nabumetone Transdermal Delivery for Treatment of Arthritis

Jagdale, Swati; Deore, Gokul K; Chabukswar, Anuruddha R.

doi:10.2174/1872211312666180227091059

Cited by 16 publications

(18 citation statements)

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“…Some advantages offered by ME include high drug solubilization capacity, enhancement of skin permeation for both hydrophobic and hydrophilic drugs, easy manufacturing, and a prolonged shelf life [21,22]. In 2018, the entrapping of NA in ME has been proposed by Jagdale et al [23] to optimize transdermal micro-emulgel delivery of the drug for the treatment of arthritis.…”

Section: Introductionmentioning

confidence: 99%

Gel Formulation of Nabumetone and a Newly Synthesized Analog: Microemulsion as a Photoprotective Topical Delivery System

et al. 2020

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Photostability studies were performed on topical formulations containing the anti-inflammatory drug Nabumetone and an analog newly synthesized in order to achieve better photostability and pharmacokinetic profile. Stability tests, according to the International Conference on Harmonization rules, were applied on ethanol solutions and topical gel formulations of both compounds. The photodegradation profiles were monitored by Multivariate curve resolution applied to the UV spectral data. The inclusion of the compounds in microemulsion was investigated to improve light stability and, at the same time, to ensure a sustained release system for skin delivery. All the formulations in solution, gel, microemulsion, and microemulsion-in-gel were exposed to a forced irradiation of 350 W/m2, corresponding to a 21 kJ/m2 min, for up to 300 min. Photostability increased significantly for both drugs in the liquid microemulsion and microemulsion-in-gel, compared to the ethanol solution and plain gel, reaching a residual drug of 97% and 98% for Nabumetone and analog in microemulsion-in-gel, respectively. Permeation experiments on the microemulsion-in-gel showed a better performance of the analog formulated at 0.2%, compared to the same formulation of Nabumetone at 0.7%. These results highlight the potential of the designed matrices as delayed drug delivery systems along with the use of lower drug doses leading to reduced side effects.

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Section: Introductionmentioning

confidence: 99%

Gel Formulation of Nabumetone and a Newly Synthesized Analog: Microemulsion as a Photoprotective Topical Delivery System

et al. 2020

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“…The general dividing line between stable and unstable colloidal dispersion is taken at either +30 or -30 mV. In this case, the values suggest that formulation possess good physical stability and particle aggregation may not occur due to electrostatic or steric repulsion between the particles [18]. Scanning electron microscopy.…”

Section: Characterization Of Slnmentioning

confidence: 99%

Transdermal delivery of solid lipid nanoparticles of ketoprofen for treatment of arthritis

Chabukswar

2019

Lett Appl NanoBioSci

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Ketoprofen (KP) is a 2-(3-benzolphenyl) propionic acid with anti-inflammatory, analgesic and antipyretic properties. It belongs to BCS Class II drug. It also has a short half-life of 120 minutes. Drugs acidic nature causes gastric irritation which is a major limitation. The present work aims to develop and evaluate solid lipid nanoparticles (SLN) to provide transdermal drug delivery. SLN loaded gel will enhance the solubility of Ketoprofen thereby increasing bioavailability giving controlled drug release. Solid lipid nanoparticles were prepared by solvent injection followed by probe sonication method. Cetyl palmitate was used as lipid and Tween80 as a surfactant. Batches were prepared by varying the concentration of the lipid phase and the surfactant phase. The solid lipid nanoparticles were evaluated for particle size analysis, drug entrapment efficiency, zeta potential and in vitro drug release study. Differential scanning calorimetry (DSC) and Powder X-ray diffraction (PXRD) study were done to study crystallinity behavior.SLN was studied for its anti-inflammatory activity. F4 batch of SLN was incorporated into gel and evaluated for drug content, pH, viscosity, in-vitro diffusion and ex-vivo diffusion study. SLN were successfully prepared. Among the batches F1-F9, F4 batch was selected based upon the size, entrapment efficiency, stability and drug release. The resultant solid lipid nanoparticles showed entrapment efficiency of 78.24%. The solubility was improved by 50 fold. The particle size was 250 nm, PDI was 0.398 and zeta potential -21.98mV. In-vitro drug release of gel from F4 SLN batch showed controlled drug release in 8 hours. Transdermal delivery of SLN retaining its anti-inflammatory activity was successfully developed.

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“…Although the metabolic process rate helps to prolong the anti-inflammatory effect, it is reasonable to assume that only a residual amount of the unmodified prodrug still circulates until its conversion is complete. The use of NB has been also proposed for topical application, often by a controlled absorption favored by opportunely designed formulations [ 34 , 35 , 36 ]. In fact, while the lipophilic nature of NB should allow sufficient epidermal crossing and tissues infiltration, only the inclusion of the drug molecules into special carriers, for example microemulgel systems, would guarantee almost complete skin absorption [ 35 ].…”

Section: Introductionmentioning

confidence: 99%

“…The use of NB has been also proposed for topical application, often by a controlled absorption favored by opportunely designed formulations [ 34 , 35 , 36 ]. In fact, while the lipophilic nature of NB should allow sufficient epidermal crossing and tissues infiltration, only the inclusion of the drug molecules into special carriers, for example microemulgel systems, would guarantee almost complete skin absorption [ 35 ]. A further opportunity for the prodrug to persist somewhat longer into blood circulation would be represented by depot injection formulations.…”

Section: Introductionmentioning

confidence: 99%

Toward Multitasking Pharmacological COX-Targeting Agents: Non-Steroidal Anti-Inflammatory Prodrugs with Antiproliferative Effects

et al. 2021

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The antitumor activity of certain anti-inflammatory drugs is often attributed to an indirect effect based on the inhibition of COX enzymes. In the case of anti-inflammatory prodrugs, this property could be attributed to the parent molecules with mechanism other than COX inhibition, particularly through formulations capable of slowing down their metabolic conversion. In this work, a pilot docking study aimed at comparing the interaction of two prodrugs, nabumetone (NB) and its tricyclic analog 7-methoxy-2,3-dihydro-1H-cyclopenta[b]naphthalen-1-one (MC), and their common active metabolite 6-methoxy-2-naphthylacetic acid (MNA) with the COX binding site, was carried out. Cytotoxicity, cytofluorimetry, and protein expression assays on prodrugs were also performed to assess their potential as antiproliferative agents that could help hypothesize an effective use as anticancer therapeutics. Encouraging results suggest that the studied compounds could act not only as precursors of the anti-inflammatory metabolite, but also as direct antiproliferative agents.

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Development of Microemulsion Based Nabumetone Transdermal Delivery for Treatment of Arthritis

Abstract: Nabumetone microemulgel exhibiting good in-vitro and ex-vivo controlled drug release was optimized.

Cited by 16 publications

References 0 publications

Gel Formulation of Nabumetone and a Newly Synthesized Analog: Microemulsion as a Photoprotective Topical Delivery System

Gel Formulation of Nabumetone and a Newly Synthesized Analog: Microemulsion as a Photoprotective Topical Delivery System

Transdermal delivery of solid lipid nanoparticles of ketoprofen for treatment of arthritis

Toward Multitasking Pharmacological COX-Targeting Agents: Non-Steroidal Anti-Inflammatory Prodrugs with Antiproliferative Effects

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