Development of solid self-nanoemulsifying granules (SSNEGs) of ondansetron hydrochloride with enhanced bioavailability potential

Beg, Sarwar; Jena, Sidharth Sankar; Patra, Chinam Niranjan; Rizwan, Mohammad; Swain, Sanjit Kumar; Jammula, Sruti; Rao, Muddana Eswara Bhanoji; Singh, Bhupinder

doi:10.1016/j.colsurfb.2012.06.031

Cited by 109 publications

(49 citation statements)

References 41 publications

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“…In vitro drug release studies showed more than 80% drug release in initial 15 min and complete drug release was observed within 30 min. This was attributed due to solubility enhancement by selected lipidic excipients (29). Figure 6 represents the globule size distribution of liquid SNEDDS were found to be within the nanometric range (56-91 nm).…”

Section: Characterization Of Sneddsmentioning

confidence: 99%

Development, Optimization, and Characterization of Solid Self-Nanoemulsifying Drug Delivery Systems of Valsartan Using Porous Carriers

et al. 2012

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Abstract. The present studies entail formulation development of novel solid self-nanoemulsifying drug delivery systems (S-SNEDDS) of valsartan with improved oral bioavailability, and evaluation of their in vitro and in vivo performance. Preliminary solubility studies were carried out and pseudoternary phase diagrams were constructed using blends of oil (Capmul MCM), surfactant (Labrasol), and cosurfactant (Tween 20). The SNEDDS were systematically optimized by response surface methodology employing 3 3-Box-Behnken design. The prepared SNEDDS were characterized for viscocity, refractive index, globule size, zeta potential, and TEM. Optimized liquid SNEDDS were formulated into free flowing granules by adsorption on the porous carriers like Aerosil 200, Sylysia (350, 550, and 730) and Neusilin US2, and compressed into tablets. In vitro dissolution studies of S-SNEDDS revealed 3-3.5-fold increased in dissolution rate of the drug due to enhanced solubility. In vivo pharmacodynamic studies in Wistar rats showed significant reduction in mean systolic BP by S-SNEDDS vis-à-vis oral suspension (p<0.05) owing to the drug absorption through lymphatic pathways. Solid-state characterization of S-SNEDDS using FT-IR and powder XRD studies confirmed lack of any significant interaction of drug with lipidic excipients and porous carriers. Further, the accelerated stability studies for 6 months revealed that S-SNEDDS are found to be stable without any change in physiochemical properties. Thus, the present studies demonstrated the bioavailability enhancement potential of porous carriers based S-SNEDDS for a BCS class II drug, valsartan.

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Section: Characterization Of Sneddsmentioning

confidence: 99%

Development, Optimization, and Characterization of Solid Self-Nanoemulsifying Drug Delivery Systems of Valsartan Using Porous Carriers

et al. 2012

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“…Capmul MCM) and emulgent (i.e. Nikkol HCO-50), which help in circumnavigation of the hepatic firstpass effect, gut wall metabolism by Cytochrome P450 enzymes and facilitated absorption of drug through intestinal lymphatic pathways (Nanjwade et al, 2011;Beg et al, 2013). Moreover, the enhanced absorption potential S-SNEDDS could also be attributed to characteristic increase in solubility of the drug, as well as burst release in gastrointestinal milieu, leading eventually to faster drug absorption (Taha et al, 2009).…”

Section: Discussionmentioning

confidence: 99%

QbD-based systematic development of novel optimized solid self-nanoemulsifying drug delivery systems (SNEDDS) of lovastatin with enhanced biopharmaceutical performance

et al. 2014

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(2015) QbD-based systematic development of novel optimized solid self-nanoemulsifying drug delivery systems (SNEDDS) of lovastatin with enhanced biopharmaceutical performance, Drug Delivery, 22:6, 765-784, DOI: 10.3109/10717544.2014 AbstractOf late, solid self-nanoemulsifying drug delivery systems (S-SNEDDS) have been extensively sought-after owing to their superior portability, drug loading, stability and patient compliance. The current studies, therefore, entail systematic development, optimization and evaluation (in vitro, in situ and in vivo) of the solid formulations of (SNEDDS) lovastatin employing rational quality by design (QbD)-based approach of formulation by design (FbD). The patient-centric quality target product profile (QTPP) and critical quality attributes (CQAs) were earmarked. Preformulation studies along with initial risk assessment facilitated the selection of lipid (i.e. Capmul MCM), surfactant (i.e. Nikkol HCO-50) and co-surfactant (i.e. Lutrol F127) as CMAs for formulation of S-SNEDDS. A face-centered cubic design (FCCD) was employed for optimization using Nikkol-HCO50 (X 1 ) and Lutrol-F127 (X 2 ), evaluating CQAs like globule size, liquefaction time, emulsification time, MDT, dissolution efficiency and permeation parameter. The design space was generated using apt mathematical models, and the optimum formulation was located, followed by validation of the FbD methodology. In situ SPIP and in vivo pharmacodynamic studies on the optimized formulation carried out in unisex Wistar rats, corroborated superior drug absorption and enhanced pharmacodynamic potential in regulating serum lipid levels. In a nutshell, the present studies report successful QbD-oriented development of novel oral S-SNEDDS of lovastatin with distinctly improved biopharmaceutical performance.

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“…Thermal findings have been combined with data from isothermal stress testing (IST), Fourier transform infrared spectroscopy (FTIR), X-ray powder diffraction (XRPD), optical and electron microscopy, among other techniques, with a view to clarifying more concisely the occurrence of drug-excipient interactions [30][31][32][33][34]. The combination of some of these techniques has been shown the occurrence of relevant drug-lipid interactions [35][36][37][38].…”

Section: Introductionmentioning

confidence: 98%

Evaluation of carvedilol compatibility with lipid excipients for the development of lipid-based drug delivery systems

Silva

Teixeira

Serpa

et al. 2015

J Therm Anal Calorim

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Carvedilol (CARV) is a widely used non-selective b-blocker, which has shown low bioavailability after oral administration (20 %) due to its low water solubility and intense first-pass metabolism. Lipid-based drug delivery systems have been proposed to improve CARV oral bioavailability. An evaluation of drug-excipient compatibility is needed to clarify potential physical and chemical interactions between them and therefore guarantee a correct selection of excipients. However, to date there are no reports on the systematic evaluation of CARV-lipid excipient compatibility. Thus, the aim of this study was to evaluate the compatibility of CARV with the lipid excipients commonly used for the development of lipid-based formulations. Thermal analysis techniques (DTA and TG/DTG), Fourier transform infrared spectroscopy and isothermal stress testing (IST) were used for this purpose. The results of this study showed that 4 of the 10 lipid excipients studied were incompatible with CARV. The strongest thermal and spectroscopic modifications were observed in CARV mixtures with oleic acid, lauric acid, lauroyl polyoxylglycerides (Gelucire Ò 44/14) and glyceryl caprylate/caprate (Capmul Ò MCM). In addition, these mixtures resulted in significant decreases in drug content after aging. On the other hand, palmitic acid, stearic acid, glyceryl behenate (Compritol ATO Ò 188), tribeheninPEG (Emulium Ò 22), polyglyceryl-6-isostearate (Plurol Isostearique Ò ) and diethylene glycol monoethyl ether (Transcutol HP Ò ) were considered good candidates for developing self-emulsifying drug delivery systems and for preparing lipid microparticle or nanoparticle containing CARV. These findings denote the relevance of combining thermal and spectroscopic techniques with thermal stress testing for the accurate determination of druglipid excipient compatibility.

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Development of solid self-nanoemulsifying granules (SSNEGs) of ondansetron hydrochloride with enhanced bioavailability potential

Cited by 109 publications

References 41 publications

Development, Optimization, and Characterization of Solid Self-Nanoemulsifying Drug Delivery Systems of Valsartan Using Porous Carriers

Development, Optimization, and Characterization of Solid Self-Nanoemulsifying Drug Delivery Systems of Valsartan Using Porous Carriers

QbD-based systematic development of novel optimized solid self-nanoemulsifying drug delivery systems (SNEDDS) of lovastatin with enhanced biopharmaceutical performance

Evaluation of carvedilol compatibility with lipid excipients for the development of lipid-based drug delivery systems

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