Browsing by Author "Achint Jain"

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Diacerein protects against iodoacetate-induced osteoarthritis in the femorotibial joints of rats
(Nanjing Medical University, 2015) Achint Jain; Royana Singh; Saurabh Singh; Sanjay Singh
The present study was undertaken to investigate the effect of diacerein on the histopathology of articular cartilage and subchondral bone of the femorotibial joint in rats. Osteoarthritis was induced in rats after single intra-articular injection of sodium iodoacetate. Rats were sacrificed 1, 2, 4, and 8 weeks post intra-articular injection to evaluate the progression of histopathogenesis of osteoarthritis. Diacerein was orally administered (15 mg/kg) once daily post 1 and 2 weeks of iodoacetate injection in two groups, respectively, for up to 12 weeks. Articular cartilage and subchondral bone of the rats of both groups were examined after 8 and 12 weeks, respectively. Quantitative histological analyses were performed by scoring these sections as per the OARSI system. Chondroitin sulfate was also estimated in articular cartilage by decrease in absorbance of methylene blue on complexation with chondroitin sulfate using a spectrophotometer. Intra-articular injection of iodoacetate induced loss of articular cartilage with progressive subchondral bone sclerosis and degeneration. Based on histopathological and biochemical findings, diacerein treatment showed chondroprotective effect. Furthermore, the chondroprotective effect of diacerein was found to be more pronounced after 12 weeks as compared to 8 weeks in both cases (i.e., post 1 and 2 weeks of iodoacetate injection). Similar results were observed by investigation of chondroitin sulfate during biochemical study, showing the chondroprotective effect. In conclusion, diacerein exhibits chondroprotective effect in rats with late onset of action. © 2015 by the Journal of Biomedical Research.
Effect of lipid matrix on repaglinide-loaded solid lipid nanoparticles for oral delivery
(Newlands Press Ltd, 2010) Manoj K Rawat; Achint Jain; Amit Mishra; Madaswamy S Muthu; Sanjay Singh
Aim: To study the effect of different types of lipid on the entrapment efficiency (EE) and physical stability of repaglinide (RG)-loaded solid lipid nanoparticles (SLNs). RG-loaded SLNs were prepared by modified solvent injection method using stearic acid (RSA), glycerol monosteratae (RGM), glyceryl behenate (RGB) and tristearin (RTS). Poloxamer F68 was used as a stabilizer. Results: SLNs were characterized by particle size, zeta-potential, EE, in vitro release, solid-state properties (differential scanning calorimetry, transmission electron microscopy and electron diffraction) and stability at 30°C/65% relative humidity for 3 months. The mean particle size and zeta-potential of RG-loaded SLNs prepared with different lipids in varying concentrations ranged from 150 to 355 nm and -21.04 ± 3.10 to -30.54 ± 2.76 mV, respectively. Conclusion: EE was found to vary with lipids in the following order: RSA < RGM < RGB < RTS. Tristearin-prepared SLNs showed a significant prolonged drug release up to 24 h. Differential scanning calorimetry and electron diffraction microphotograph results indicated that RG entrapped in the SLNs existed in an amorphous or molecular state. SLNs prepared with stearic acid, glycerol monostearate and glyceryl behenate after storage showed significant increases in particle size, polydispersity index and EE. The SLNs prepared with tristearin were stable. © 2010 Future Science Ltd.
In vitro and in vivo evaluation of buccal bioadhesive films containing salbutamol sulphate
(2010) Sanjay Singh; Rajeev Soni; Manoj Kumar Rawat; Achint Jain; Shripad Bheemrao Deshpande; Sanjeev Kumar Singh; Madaswamy Sona Muthu
The aim of present study was to prepare and evaluate buccal bioadhesive films of salbutamol sulphate (SS) for the treatment of asthma. The films were designed to release the drug for a prolonged period of time so as to reduce the frequency of administration of the available conventional dosage forms of SS. The different proportions of sodium carboxymethylcellulose (SCMC) and Carbopol 940P (CP 940P) were used for the preparation of films. Carbopol was used to incorporate the desired bioadhesiveness in the films. The films were prepared by solvent casting method and evaluated for bioadhesion, in vitro drug release and anti asthmatic effect (bronchoprotection) in histamine induced bronchospasm of guinea pigs. In vitro drug release from the film was determined using a modified Franz diffusion cell while bioadhesiveness was evaluated with a modified two-arm balance using guinea pig buccal mucosa as a model tissue. Films containing SCMC : CP 940P ratio of 76 : 24 was found to be the best with moderate swelling along with favorable bioadhesion force and in vitro drug release. The drug release mechanism was found to follow non-Fickian diffusion as release mechanism. The prolonged in vivo effect (bronchoprotection) obtained from the buccal bioadhesive film of SS administered via buccal route may improve the treatment of asthmatic disorders by reducing the frequency of administration which is associated with the tolerance effect of SS. Additionally for the clinical benefit, it is also expected to reduce the major adverse effects of SS such as tachycardia and arrhythmias via buccal absorption. © 2010 Pharmaceutical Society of Japan.
Mucoadhesive gel containing immunotherapeutic nanoparticulate satranidazole for treatment of periodontitis: Development and its clinical implications
(Royal Society of Chemistry, 2015) Yuvraj Singh; Parameswara R. Vuddanda; Achint Jain; Sarita Parihar; Thakur P. Chaturvedi; Sanjay Singh
The aim of this study was to alleviate shortcomings in periodontal treatment by utilizing a mucoadhesive gel containing immunotherapeutic ganglioside coated polymeric nanoparticles (G-PNP) bearing satranidazole (SZ). Nanoprecipitation was used to fabricate SZ loaded G-PNP. In our previous deliberations aqueous dispersibility of conventional SZ had raised dose consistency issues. Usage of G-PNP allayed those fears as DSC and XRD data showed that SZ was rendered amorphous (more water dispersible than crystalline SZ) when captured in a polymeric matrix of nanoparticles. G-PNP were added to sodium carboxy methyl cellulose (SCMC 30 NP) gels and compared against SCMC 30 (gel containing conventional SZ) for texture, mucoadhesion, drug release and inhibitory susceptibility of Aggregatibacter actinomycetomicans. Subsequently a 21 day single blind clinical trial comparing the efficacy of SCMC 30 NP and SCMC 30 was conducted. SCMC 30 NP showed a maximum mucoadhesion force (43.27 ± 4.10 gf), low hardness (12.28 ± 0.17 N), moderate gel strength (8.53 ± 0.21 N) and elasticity (5.50 ± 0.03 mm). 'Well' diffusion data revealed qualitatively greater antibacterial activity of SCMC 30 NP. Dissolution studies demonstrated diffusion controlled release of SZ at concentrations above MIC. SCMC 30 NP caused a significant (P < 0.05) decrease in clinical markers of periodontitis, i.e. gingival index and pocket depth as compared to SCMC 30. Also reduction in the plaque index produced by SCMC 30 NP was highly significant (P < 0.01) as compared to SCMC 30 at the end of the 21st day of clinical study. Amelioration of disease was improved due to Th-2 biased immuno shifting mediated by G-PNPs, which increased secretion of anti-inflammatory cytokines like IL-4 and TGF-β from J774 macrophages. Clinical benefits incurred along with ease of application calls for a scaled up investigation of SCMC 30 NP. © The Royal Society of Chemistry 2015.
Targeting of diacerein loaded lipid nanoparticles to intra-articular cartilage using chondroitin sulfate as homing carrier for treatment of osteoarthritis in rats
(Elsevier Inc., 2014) Achint Jain; Sandeep Kumar Mishra; Parameswara Rao Vuddanda; Sanjay Kumar Singh; Royana Singh; Sanjay Singh
Targeted delivery of antiosteoarthritic drug diacerein to articular tissue could be a major achievement and soluble polysaccharide chondroitin sulfate (ChS) may be a suitable agent for this. Therefore, diacerein loaded solid lipid nanoparticles modified with ChS (ChS-DC-SLN) were prepared for synergistic effect of these agents to combat multidimensional pathology of osteoarthritis (OA). Prepared formulation were of size range 396. ±. 2.7. nm, showed extended release up to 16. h and increased bioavailability of diacerein by 2.8 times. ChS-DC-SLN were evaluated for their effect on histopathology of femoro-tibial joint of rat knee and amount of ChS and rhein (an active metabolite of diacerein) at targeted site. Concentration of rhein was significantly higher in case of ChS-DC-SLN (7.8. ±. 1.23. μg/ml) than that of drug dispersion (2.9. ±. 0.45. μg/ml). It can be stated that ChS served as homing to articular cartilage for targeting of drug. Thus, ChS-DC-SLN have great potential to enhance the overall efficacy of treatment for OA. From the Clinical Editor: This study demonstrates the feasibility of targeted delivery of diacerein to articular tissue using soluble polysaccharide chondroitin sulfate as the targeting vector. This approach has the potential to significantly increase anti-arthritic drug concentration in joints without leading to systemic toxicity. © 2014 Elsevier Inc.