Development and Characterization of Self-Nanoemulsifying Drug Delivery Systems (SNEDDS) of Atorvastatin Calcium

Mantri, Shiva Kumar; Pashikanti, Shailaja; Murthy, K. Srikanta

doi:10.2174/156720112800234594

Cited by 9 publications

(5 citation statements)

References 13 publications

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“…The transmittance of the resulting dispersions up on diluting 25 mg of the formulations with 50 mL distilled water was measured using UV spectrophotometer at 600 nm. The area of nano emulsification region was identified as described above by constructing pseudo-ternary phase diagrams 9 .…”

Section: Effect Of Pomalidomide Loadingmentioning

confidence: 99%

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2022

IJPSR

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Background: Pomalidomide belongs to BCS class IV drug with low solubility and undergoes first-pass metabolism leads to reduced bioavailability of 15%. Objective: The current study aimed to develop pomalidomide Super saturable-SNEDDS to enhance solubility. Methods: Preliminary solubility studies were performed to identify oil, surfactant, and co-surfactant ratios. Pseudo tertiary phase diagram constructed to select the areas of nanoemulsion and based on monophasic region. Nineteen ratios were selected for drug loading study having oil: Smix ratio in 3:1, from which 15 formulations of pomalidomide SNEDDS were prepared with 4mg drug loading and screened for visual observation and turbidity measurement studies. These SNEDDS are further characterized for robustness, content of drug, entrapment efficiency, and in-vitro dissolution analysis. The optimized SNEDDS formulation was selected for screening of precipitation inhibitor by adding 2% precipitation inhibitors, and concentration-time profiles were studied under non-sink conditions from which best PI was selected and then in-vitro dissolution studies conducted for the super saturable SNEDDS (S-SNEDDS). The optimized final formulation S-SNEDDS with the highest drug release was analyzed for FTIR, particle size, Z average, zeta potential, SEM analysis, and stability studies. Results: Based on pseudo tertiary phase diagram, Akomed E oil -Caprol PGE 860 -and PEG 600 as oil, surfactant, and co-surfactant selected, respectively. All the formulations were stable with no phase separation and maximum % transmittance. The formulation F11 was selected as optimized one based on maximum drug release of 99.04% within 60 min. By adding PVP K17 as a precipitation inhibitor to conventional SNEDDS, a super saturable system was prepared. Firstly, the prepared SNEDDS played an important role in increasing the aqueous solubility and hence oral absorption due to nano-range size. Secondly, the S-SNEDDS found to be advantageous over SNEDDS for having a higher drug load and inhibition of dilution precipitation of pomalidomide. Formulated S-SNEDDS (F11) showed drug release of 99.98%. The particle size, PDI and zeta potential of the optimized formulation F11 S-SNEDDS were 49.0 nm, 0.318, and -24.4 mV, respectively. The FTIR and SEM studies did not indicate any drug excipient interaction and confirmed nanosized which is stable. Conclusion: Pomalidomide-loaded S-SNEDDS could potentially be exploited as a delivery system for improving solubility and increase drug release.. INTRODUCTION:Pomalidomide, an analog structurally similar to thalidomide, is an immunemodulatory agent with antineoplastic activity. In in-vitro cellular assays, pomalidomide inhibited QUICK RESPONSE CODE

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Section: Effect Of Pomalidomide Loadingmentioning

confidence: 99%

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2022

IJPSR

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“…The oil was added to the mixture and vortexed for 2 min. 25 mg of the formulations diluted using 50 mL distilled water and evaluated for % transmission spectrophotometrically 10 .…”

Section: Effect Of Doravirine Loadingmentioning

confidence: 99%

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2022

IJPSR

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Doravirine is an HIV-1 non-nucleoside reverse transcriptase inhibitor (NNRTI). The aim of the present investigation was to develop a selfnanoemulsifying drug delivery system (SNEDDS) to enhance the solubility and dissolution of poorly water-soluble doravirine. The solubility of doravirinein various oils was determined to identify the oil phase of SNEDDS. Various surfactants and co-surfactants were screened for their ability to emulsify the selected oil. A ternary phase diagram was constructed to identify the efficient self-emulsifying region. The optimized SNEDDS formulation (F8) contained drug (100 mg), neobee M5 (22.2%), caproic acid (58.2%) and PEG 600 (19.4%). The SNEDDS was further evaluated for its robustness, turbidity, % drug content, entrapment efficiency, droplet size, and zeta potential. The optimized formulation of drug-loaded SNEDDS exhibited 98% entrapment efficiency, 99% drug content and 99% in-vitro drug release in 60 min as compared with the plain drug, which had a limited dissolution rate (31%). The particle size for the optimized formulation of SNEDDS (F8) was found to be 67.8 nm with PDI 0.173. The negative value of zeta potential of -23.2 mV might be due to anionic groups of free fatty acids and glycol present in the oil, surfactant, and cosurfactant. The degradation of doravirine from optimized doravirine SNEDDS formulation was significantly less when compared to the pure drug degradation. These results suggest the potential use of SNEDDS to improve dissolution and stability of poorly water-soluble doravirine. INTRODUCTION:The oral route is the easiest and most convenient way of noninvasive administration. However, oral drug delivery may hamper drug molecules that exhibit poor aqueous solubility. Approximately 40% of the new chemical entities exhibit poor aqueous solubility and present a major challenge to the modern drug delivery system, which leads to poor oral bioavailability, high intra-, and inter-subject variability and lack of dose proportionality.

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“…The stability of DFX loaded SNEDDS formulations in different pH buffer solutions (pH 1.2, Ph4.5, pH 6.8 and, pH 7.4) was checked by 100-fold dilution in each of the buffer solutions, then subjected to droplet size and PDI measurements by ZetaSizer (Malvern 1000 HS, Worcestershire ® , UK), and the values were compared with droplet size and PDI that resulted from dispersions in purified water [46].…”

Section: Effect Of Ph Of the Dispersion Media On Droplet Size And Pdimentioning

confidence: 99%

A Solid Ultra Fine Self-Nanoemulsifying Drug Delivery System (S-SNEDDS) of Deferasirox for Improved Solubility: Optimization, Characterization, and In Vitro Cytotoxicity Studies

et al. 2020

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The research work was designed to develop a solid self-nanoemulsifying drug delivery system (S-SNEDDS) of deferasirox (DFX). According to the solubility studies of DFX in different components, Peceol, Kolliphor EL, and Transcutol were selected as excipients. Pseudo-ternary phase diagrams were constructed, and then SNEDDS formation assessment studies and solubility of DFX in selected SNEDDSs formulations were performed. DFX loaded SNEDDS were prepared and characterized. The optimum DFX-SNEDDS formulations were developed. The relative safety of the optimized SNEDDS formulation was examined in a human immortalized myelogenous leukemia cell line, K562 cells, using the MTT cell viability test. Cytotoxicity studies revealed more cell viability (71.44%) of DFX loaded SNEDDS compared to pure DFX (3.99%) at 40 μM. The selected DFX-SNEDDS formulation was converted into S-SNEDDS by adsorbing into porous carriers, in order to study its dissolution behavior. The in vitro drug release studies indicated that DFX release (Q5%) from S-SNEDDS solidified with Neusilin UFL2 was significantly higher (93.6 ± 0.7% within 5 min) compared with the marketed product (81.65 ± 2.10%). The overall results indicated that the S-SNEDDS formulation of DFX could have the potential to enhance the solubility of DFX, which would in turn have the potential to improve its oral bioavailability as a safe novel delivery system.

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Development and Characterization of Self-Nanoemulsifying Drug Delivery Systems (SNEDDS) of Atorvastatin Calcium

Cited by 9 publications

References 13 publications

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A Solid Ultra Fine Self-Nanoemulsifying Drug Delivery System (S-SNEDDS) of Deferasirox for Improved Solubility: Optimization, Characterization, and In Vitro Cytotoxicity Studies

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