Impact of solidification on micromeritic properties and dissolution rate of self-nanoemulsifying delivery system loaded with docosahexaenoic acid

Ghosh, Dipanjoy; Singh, Sachin Kumar; Khursheed, Rubiya; Pandey, Narendra Kumar; Kumar, Bimlesh; Kumar, Rajan; Kumari, Yogita; Kaur, Gurpreet; Ayinkamiye, Clarisse; Awasthi, Ankit; Gulati, Monica; Jain, Subheet Kumar; Porwal, Omji; Bayrakdar, Esra; Sheet, Muath; Kuppusamy, Gowthamarajan; Gupta, Saurabh; Corrie, Leander; Gunjal, Pradnya; Gupta, Rajneesh Kumar; Singh, Thakur Gurjeet; Sinha, Shibanand

doi:10.1080/03639045.2020.1742143

Cited by 26 publications

(8 citation statements)

References 28 publications

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“…Emulsion droplet size (PS) is an important index that reflects the rate and extent of drug release and consequently its absorption [44]. A good correlation was noticed between the oil content and the droplet size within the formulae.…”

Section: Discussionmentioning

confidence: 99%

Design and Optimization of Pioglitazone Hydrochloride Self-Nanoemulsifying Drug Delivery System (SNEDDS) Incorporated into an Orally Disintegrating Tablet

et al. 2022

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Pioglitazone Hydrochloride (PGZ) suffers from poor aqueous solubility. The aim of this research was to design orally disintegrating tablets with self-nanoemulsifying properties (T-SNEDDS) to improve the Pioglitazone solubility and dissolution rate. Three liquid self-nanoemulsifying systems (L-SNEDDS) were formulated and evaluated for transmittance percentage, emulsification time, particle size, Poly dispersity index (PDI), percentage of content, solubility and stability. The optimum L-SNEDDS formula was converted to a solidified self-nanoemulsifying drug delivery system (S-SNEDDS) by adsorption on Syloid (SYL). Powder characterization tests, such as flowability tests, differential scanning calorimetry (DSC), Fourier transform infrared spectroscopy (FTIR), X-ray diffraction (XRD) and scanning electron microscopy (SEM), were performed for the selected S-SNEDDS formulation. Orally disintegrating tablets (ODT) were formulated by blending S-SNEDDS with tableting excipients. The ODT tablet batch composed of Prosolv was selected for tablet quality control tests, such as hardness, friability, disintegration time, content uniformity, weight variation, in vitro release, in vivo studies and accelerated stability studies. ODT tablets showed accepted mechanical properties and rapid disintegration time (<30 s). No drug degradation was observed at 3 months into the accelerated stability study. The optimized L-SNEDDS, S-SNEDDS and ODT (T-SNEDDS), showed significant enhancement of PGZ in vitro dissolution profiles compared to the pure drug (p > 0.05). In vivo pharmacokinetic and pharmacodynamic evaluation of ODTs showed better behavior compared to the raw drug suspension and the commercial tablet (p > 0.05). Orally disintegrating tablets revealed a promising potential to improve Pioglitazone poor aqueous solubility, dissolution profile and bioavailability.

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Section: Discussionmentioning

confidence: 99%

Design and Optimization of Pioglitazone Hydrochloride Self-Nanoemulsifying Drug Delivery System (SNEDDS) Incorporated into an Orally Disintegrating Tablet

et al. 2022

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“…Three different solid carriers were used: Neusilin ® , US2, Neusilin ® UFL2 (Fuji Chemical, Tokyo, Japan), and Syloid ® XDP 3150 (Grace, Columbia, Maryland, USA) for preparing different batches of DFX-S-SNEDDS formulations. The oil adsorption capacity was measured for each solid carrier, which is defined as the amount of porous carrier required for transforming the unit dose of liquid oily formulation into the solid free flowing powder [48]. The 200 mg of each carrier was placed separately in a mortar and the formulation P5-40 was added drop wisely with good mixing after each addition until a non-sticky free flowing powder was obtained and the weight of P5-40 formulation used was recorded [49].…”

Section: Development Of Dfx Loaded Solid-snedds (S-snedds)mentioning

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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“…For individuals that have swallowing problems, ODTs are very beneficial [2][3][4]. The disintegrate time of ODTs is within a minute and is suitable for patients with dysphasia [5,6]. ODTs have high bioavailability because as the saliva passes down the stomach, the absorption of some drugs from the mouth, pharynx, and esophagus follows.…”

Section: Introductionmentioning

confidence: 99%

Development and Characterization of Oro-Dispersible Tablets of Metformin Hydrochloride Using Cajanus Cajan Starch as a Natural Superdisintegrant

et al. 2022

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Objective: The aim of the research work was to explore the use of Cajanus cajan (Pigeon pea) polysaccharide as a superdisintegrant. The novel superdisintegrant has been evaluated for its action by incorporating it into orodispersible tablets of Metformin Hydrochloride. Methods: Cajanus cajan starch was extracted from its seeds and superdisintegrant was developed by microwave modification of the extract. Various characterization tests such as gelatinization temperature, water absorption index, pH, and viscosity were used to identify the microwave-modified polysaccharide. The orodispersible tablets were made using a direct compression process employing varying concentrations of modified Cajanus cajan starch. Prepared tablets were tested for several pre and post-compression parameters and compared with a well-established synthetic superdisintegrant, sodium starch glycolate. The stability studies were conducted on an optimized formulation. Results: Fourier transform infrared spectroscopy study showed that the drug had no interactions with the microwave-modified Cajanus cajan starch. SEM confirmed that Cajanus cajan starch granules exhibited intact granular structure in oval shapes and smooth surfaces. After microwave modification, the Cajanus cajan starch component lost its granular structure, which further led to the generation of surface pores and internal channels, causing overall swelling responsible for superdisintegrant activity. The optimized formulation (ODF5) containing 15 % modified Cajanus cajan starch performed better in terms of wetting time (22.21 s), disintegration time (53.3 s), and in vitro drug release (92%), as compared to formulation prepared by synthetic superdisintegrant (ODF1). Conclusion: The present investigation concluded that modified Cajanus cajan starch has good potential as a superdisintegrant for formulating oro-dispersible tablets. Furthermore, modified Cajanus cajan starch is inexpensive, non-toxic and compatible in comparison with available synthetic superdisintegrants.

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Impact of solidification on micromeritic properties and dissolution rate of self-nanoemulsifying delivery system loaded with docosahexaenoic acid

Cited by 26 publications

References 28 publications

Design and Optimization of Pioglitazone Hydrochloride Self-Nanoemulsifying Drug Delivery System (SNEDDS) Incorporated into an Orally Disintegrating Tablet

Design and Optimization of Pioglitazone Hydrochloride Self-Nanoemulsifying Drug Delivery System (SNEDDS) Incorporated into an Orally Disintegrating Tablet

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

Development and Characterization of Oro-Dispersible Tablets of Metformin Hydrochloride Using Cajanus Cajan Starch as a Natural Superdisintegrant

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