An Overview on Multiple Emulsions

2021 ◽  
pp. 156-162
Author(s):  
Gurunath S. Dhadde ◽  
Hanmant S. Mali ◽  
Indrayani D. Raut ◽  
Manoj M. Nitalikar
Keyword(s):  
Oral Delivery ◽  
In Vitro Release ◽  
Specific Reference ◽  
Intermediate Step ◽  
Rheological Characterization ◽  
Water Emulsion ◽  
Multiple Emulsions ◽  
Oil In Water ◽  
Wide Range

Multiple emulsions are dynamic hetero-dispersed structures in which water concurrently occurs water in oil and oil in water emulsion both controlled by lipophillic and hydrophilic surfactants. The combination of all such surfactants is useful in stabilizing multiple emulsions. Multiple emulsions include water-in-oil-in-water (w / o / w) and oil-in-water-in-oil (o / w / o) type; the former has extensive formulation, preparation techniques, and multiple-emulsion in-vitro analysis methods are checked. With specific reference to multiple emulsions of the w / o / w, different factors influencing the stability of multiple emulsions and stabilize strategies are discussed in detail. It finds wide range of applications in Multiple emulsions in cancer therapy, Multiple emulsions in herbal medicines, Vaccine / adjuvant, Oxygen replacement, Inverse targeting, Multiple diabetes emulsions, Multiple emulsions in food, Drug over doses treatment, etc. In the course of such microencapsulation a few emulsions were also used as an intermediate step in the process of such microencapsulation and are the structures of growing interest in the oral delivery of hydrophilic drugs that become unstable in gastrointestinal tracts such as proteins and peptides. Stability a with developing preparation methods, drug release tests, in vitro release studies, globule size or particle size, stability and rheological characterization of multiple emulsions, will be able to provide a novel carrier mechanism for medicines, cosmetics and pharmaceutical agents.

Fenofibrate Solid Dispersion for Improving Oral Bioavailability: Preparation, and Characterization and in vivo Evaluation

2020 ◽  
Vol 13 (5) ◽  
pp. 5102-5109
Author(s):  
Venu Madhav K ◽  
Somnath De ◽  
Chandra Shekar Bonagiri ◽  
Sridhar Babu Gummadi
Keyword(s):  
Oral Bioavailability ◽  
Oral Delivery ◽  
Solid Dispersions ◽  
In Vitro Release ◽  
Aqueous Solubility ◽  
Water Soluble ◽  
Scanning Calorimetry ◽  
In Vivo Evaluation

Fenofibrate (FN) is used in the treatment of hypercholesterolemia. It shows poor dissolution and poor oral bioavailability after oral administration due to high liphophilicity and low aqueous solubility. Hence, solid dispersions (SDs) of FN (FN-SDs) were develop that might enhance the dissolution and subsequently oral bioavailability. FN-SDs were prepared by solvent casting method using different carriers (PEG 4000, PEG 6000, β cyclodextrin and HP β cyclodextrin) in different proportions (0.25%, 0.5%, 0.75% and 1% w/v). FN-SDs were evaluated solubility, assay and in vitro release studies for the optimization of SD formulation. Differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD) and scanning electron microscopy (SEM) analysis was performed for crystalline and morphology analysis, respectively. Further, optimized FN-SD formulation evaluated for pharmacokinetic performance in Wistar rats, in vivo in comparison with FN suspension.  From the results, FN-SD3 and FN-SD6 have showed 102.9 ±1.3% and 105.5±3.1% drug release, respectively in 2 h. DSC and PXRD studies revealed that conversion of crystalline to amorphous nature of FN from FT-SD formulation. SEM studies revealed the change in the orientation of FN when incorporated in SDs. The oral bioavailability FN-SD3 and FN-SD6 formulations exhibited 2.5-folds and 3.1-folds improvement when compared to FN suspension as control. Overall, SD of FN could be considered as an alternative dosage form for the enhancement of oral delivery of poorly water-soluble FN.

Development, in vitro and in vivo Evaluations of Solid-Lipid Microparticles based on Solidified Micellar Carrier System for Oral Delivery of Cefepime

2017 ◽  
Vol 10 (1) ◽  
pp. 3582-3593
Author(s):  
Chukwuebuka Umeyor ◽  
Uchechukwu Nnadozie ◽  
Anthony Attama
Keyword(s):  
Oral Delivery ◽  
In Vitro Release ◽  
Carrier System ◽  
Solid Lipid ◽  
Solid Lipid Microparticles ◽  
Release Study ◽  
Lipid Microparticles ◽  
Vitro Release

This study seeks to formulate and evaluate a solid lipid nanoparticle-based, solidified micellar carrier system for oral delivery of cefepime. Cefepime has enjoyed a lot of therapeutic usage in the treatment of susceptible bacterial infections; however, its use is limited due to its administration as an injection only with poor patient compliance. Since oral drug administration encourage high patient compliance with resultant effect in improved therapy, cefepime was formulated as solid lipid microparticles for oral delivery using the concept of solidified micellar carrier system. The carrier system was evaluated based on particle yield, particle size and morphology, encapsulation efficiency (EE %), and thermal analysis using differential scanning calorimeter (DSC). Preliminary microbiological studies were done using gram positive and negative bacteria. In vitro release study was performed using biorelevant media, while in vivo release study was performed in white albino rats. The yield of solid lipid microparticles (SLM) ranged from 84.2 – 98.0 %. The SLM were spherical with size ranges of 3.8 ± 1.2 to 42.0 ± 1.4 µm. The EE % calculated ranged from 83.6 – 94.8 %. Thermal analysis showed that SLM was less crystalline with high potential for drug entrapment. Microbial studies showed that cefepime retained its broad spectrum anti-bacterial activity. In vitro release showed sustained release of cefepime from SLM, and in vivo release study showed high concentration of cefepime released in the plasma of study rats. The study showed that smart engineering of solidified micellar carrier system could be used to improve oral delivery of cefepime.

scholarly journals Development of Piperine-Loaded Solid Self-Nanoemulsifying Drug Delivery System: Optimization, In-Vitro, Ex-Vivo, and In-Vivo Evaluation

Nanomaterials ◽  
2021 ◽  
Vol 11 (11) ◽  
pp. 2920
Author(s):  
Ameeduzzafar Zafar ◽  
Syed Sarim Imam ◽  
Nabil K. Alruwaili ◽  
Omar Awad Alsaidan ◽  
Mohammed H. Elkomy ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Oral Delivery ◽  
Ex Vivo ◽  
In Vitro Release ◽  
System Optimization ◽  
Globule Size

Hypertension is a cardiovascular disease that needs long-term medication. Oral delivery is the most common route for the administration of drugs. The present research is to develop piperine self-nanoemulsifying drug delivery system (PE-SNEDDS) using glyceryl monolinoleate (GML), poloxamer 188, and transcutol HP as oil, surfactant, and co-surfactant, respectively. The formulation was optimized by three-factor, three-level Box-Behnken design. PE-SNEDDs were characterized for globule size, emulsification time, stability, in-vitro release, and ex-vivo intestinal permeation study. The optimized PE-SNEDDS (OF3) showed the globule size of 70.34 ± 3.27 nm, percentage transmittance of 99.02 ± 2.02%, and emulsification time of 53 ± 2 s Finally, the formulation OF3 was transformed into solid PE-SNEDDS (S-PE-SNEDDS) using avicel PH-101 as adsorbent. The reconstituted SOF3 showed a globule size of 73.56 ± 3.54 nm, PDI of 0.35 ± 0.03, and zeta potential of −28.12 ± 2.54 mV. SEM image exhibited the PE-SNEDDS completely adsorbed on avicel. Thermal analysis showed the drug was solubilized in oil, surfactant, and co-surfactant. S-PE-SNEDDS formulation showed a more significant (p < 0.05) release (97.87 ± 4.89% in 1 h) than pure PE (27.87 ± 2.65% in 1 h). It also exhibited better antimicrobial activity against S. aureus and P. aeruginosa and antioxidant activity as compared to PE dispersion. The in vivo activity in rats exhibited better (p < 0.05) antihypertensive activity as well as 4.92-fold higher relative bioavailability than pure PE dispersion. Finally, from the results it can be concluded that S-PE-SNEDDS might be a better approach for the oral delivery to improve the absorption and therapeutic activity.

Thiolated Eudragit-Coated Chitosan Microspheres as an Oral Drug Delivery System

2007 ◽  
Vol 342-343 ◽  
pp. 445-448 ◽  
Author(s):  
Ji Shan Quan ◽  
Hu Lin Jiang ◽  
Yun Jaie Choi ◽  
Mi Kyong Yoo ◽  
Chong Su Cho
Keyword(s):  
Oral Delivery ◽  
Oral Drug Delivery ◽  
In Vitro Release ◽  
Oral Drug ◽  
Average Particle ◽  
Protein Drug ◽  
Chitosan Microspheres ◽  
Oral Drug Delivery System ◽  
Cysteine Hydrochloride

The aim of this study is to prepare mucoadhesive chitosan microspheres for protein drug to deliver to intestine through oral administration. The thiolated Eudragit was synthesized by reaction between L-cysteine hydrochloride and Eudragit® L-100. About 8 mol-% of cysteine was introduced to the Eudragit-cysteine conjugate. The conjugate was used to coat bovine serum albumin (BSA)-loaded chitosan microspheres. The average particle sizes of BSA-loaded thiolated Eudragit-coated chitsoan microspheres (TECMs) were 4.06±0.74 .m and the uniform sizedistribution was shown. The in vitro release of BSA from BSA-loaded TECMs was pH-dependent. Our results indicated that thiolated Eudragit might be a good candidate as a coating material for oral delivery of protein drug owing to mucoadhesive and pH-sensitive properties.

scholarly journals Encapsulation of Olive Pomace Extract in Rocket Seed Gum and Chia Seed Gum Nanoparticles: Characterization, Antioxidant Activity and Oxidative Stability

Foods ◽  
2021 ◽  
Vol 10 (8) ◽  
pp. 1735
Author(s):  
Alican Akcicek ◽  
Fatih Bozkurt ◽  
Cansu Akgül ◽  
Salih Karasu
Keyword(s):  
Encapsulation Efficiency ◽  
In Vitro Release ◽  
Olive Pomace ◽  
Pickering Emulsions ◽  
Chia Seed ◽  
Oil In Water ◽  
Wall Materials ◽  
Seed Gum ◽  
Vitro Release

The aim of this study was to determine the potential use of rocket seed and chia seed gum as wall materials, to encapsulate and to prevent degradation of olive pomace extract (OPE) in polymeric nanoparticles, and to characterize olive pomace extract-loaded rocket seed gum nanoparticles (RSGNPs) and chia seed gum nanoparticles (CSGNPs). The phenolic profile of olive pomace extract and physicochemical properties of olive pomace, rocket seed gum (RSG), and chia seed gum (CSG) were determined. The characterization of the nanoparticles was performed using particle size and zeta potential measurement, differential scanning calorimeter (DSC), Fourier-transform infrared spectroscopy (FTIR), scanning electron microscope (SEM), encapsulation efficiency (EE%), in vitro release, and antioxidant activity analyses. Nanoparticles were used to form oil in water Pickering emulsions and were evaluated by oxitest. The RSGNPs and CSGNPs showed spherical shape in irregular form, had an average size 318 ± 3.11 nm and 490 ± 8.67 nm, and zeta potential values of-22.6 ± 1.23 and -29.9 ± 2.57, 25 respectively. The encapsulation efficiency of the RSGNPs and CSGNPs were found to be 67.01 ± 4.29% and 82.86 ± 4.13%, respectively. The OPE-RSGNP and OPE-CSGNP presented peaks at the 1248 cm−1 and 1350 cm−1 which represented that C-O groups and deformation of OH, respectively, shifted compared to the OPE (1252.53 cm−1 and 1394.69 cm−1). The shift in wave numbers showed interactions of a phenolic compound of OPE within the RSG and CSG, respectively. In vitro release study showed that the encapsulation of OPE in RSGNPs and CSGNPs led to a delay of the OPE released in physiological pH. The total phenolic content and antioxidant capacity of RSGNPs and CSGNPs increased when the OPE-loaded RSGNPs and CSGNPs were formed. The encapsulation of OPE in RSGNPs and CSGNPs and the IP values of the oil in water Pickering emulsions containing OPE-RSGNPs and OPE-CSGNPs were higher than OPE, proving that OPE-loaded RSGNPs and CSGNPs significantly increased oxidative stability of Pickering emulsions. These results suggest that the RSG and CSG could have the potential to be utilized as wall materials for nanoencapsulation and prevent degradation of cold-pressed olive pomace phenolic extract.

scholarly journals A Novel Sustained Anti-Inflammatory Effect of Atorvastatin—Calcium PLGA Nanoparticles: In Vitro Optimization and In Vivo Evaluation

Pharmaceutics ◽  
2021 ◽  
Vol 13 (10) ◽  
pp. 1658
Author(s):  
Dalia H. Abdelkader ◽  
Ahmed Kh. Abosalha ◽  
Mohamed A. Khattab ◽  
Basmah N. Aldosari ◽  
Alanood S. Almurshedi
Keyword(s):  
Particle Size ◽  
Zeta Potential ◽  
In Vitro Release ◽  
In Vivo Evaluation ◽  
Water Emulsion ◽  
Atorvastatin Calcium ◽  
Anti Inflammatory ◽  
Inflammatory Effect

Atorvastatin Calcium (At-Ca) has pleiotropic effect as anti-inflammatory drug beside its main antihyperlipidemic action. Our study was conducted to modulate the anti-inflammatory effect of At-Ca to be efficiently sustained for longer time. Single oil-water emulsion solvent evaporation technique was used to fabricate At-Ca into polymeric nanoparticles (NPs). In vitro optimization survey was performed on Poly(lactide-co-glycolide) (PLGA) loaded with At-Ca regrading to particle size, polydispersity index (PDI), zeta potential, percent entrapment efficiency (% EE), surface morphology and in vitro release pattern. In vitro drug-polymers interactions were fully scanned using Fourier-Transform Infrared Spectroscopy (FTIR) and Differential Scanning calorimetry (DSC) proving that the method of fabrication is an optimal strategy maintaining the drug structure with no interaction with polymeric matrix. The optimized formula with particle size (248.2 ± 15.13 nm), PDI (0.126 ± 0.048), zeta potential (−12.41 ± 4.80 mV), % EE (87.63 ± 3.21%), initial burst (39.78 ± 6.74%) and percent cumulative release (83.63 ± 3.71%) was orally administered in Male Sprague–Dawley rats to study the sustained anti-inflammatory effect of At-Ca PLGA NPs after carrageenan induced inflammation. In vivo results demonstrate that AT-Ca NPs has a sustained effect extending for approximately three days. Additionally, the histological examination revealed that the epidermal/dermal layers restore their typical normal cellular alignment with healthy architecture.

scholarly journals Self microemulsifying powder using Aerosil as a carrier

2021 ◽  
Vol 56 (2) ◽  
pp. 141-146
Author(s):  
N Arju ◽  
PK Bara ◽  
MT Amin ◽  
DR Bhowmik ◽  
MS Hossain
Keyword(s):  
Oral Delivery ◽  
Evaluation Studies ◽  
In Vitro Release ◽  
Study Drug ◽  
Evaluation Study ◽  
Flowing Powder ◽  
Uv Visible ◽  
Short Time ◽  
Vitro Release

This investigation highlighted the development of a solid self micro emulsifying drug delivery system (solid SMEDDS) for improved oral delivery of Valsartan. Liquid SMEDDS were formulated and then the liquid formulation was transformed into free-flowing powder by adsorption on a solid carrier. Here the formulations were prepared in various ratios of the drug to the excipients. Various evaluation studies were performed. In-vitro release profiles of all formulations were evaluated. The concentration of the diffused drug was measured using a UV-visible spectrophotometer at λmax= 250 nm. The faster dissolution was exhibited by the formulations containing Avicel. The experimental results for prepared solid-SMEDDS showed the improved dissolution of the study drug in a short time. F-3 (Assay:77%; Dissolution: 51.7% after 45 min, 63% after 60 min) and F-4 (Assay:63%; Dissolution: 49.1% after 45 min, 67% after 60 min) showed better evaluation study and this two might be formulated in future. Thus, this study revealed the formulation solid-SMEDDS using Aerosil 200 as an adsorbent with the potential of enhancing the solubility, and dissolution rate of the drug. Bangladesh J. Sci. Ind. Res.56(2), 141-146, 2021

scholarly journals Insulin-Loaded Barium Salt Particles Facilitate Oral Delivery of Insulin in Diabetic Rats

Pharmaceutics ◽  
2020 ◽  
Vol 12 (8) ◽  
pp. 710
Author(s):  
Rahela Zaman ◽  
Md. Emranul Karim ◽  
Iekhsan Othman ◽  
Anuar Zaini ◽  
Ezharul Hoque Chowdhury
Keyword(s):  
Blood Glucose ◽  
Blood Glucose Level ◽  
Glucose Level ◽  
Insulin Aspart ◽  
Oral Delivery ◽  
Diabetic Rats ◽  
Duration Of Action ◽  
Wide Range ◽  
Ft Ir

Oral delivery is considered as the most preferred and yet most challenging mode of drug administration; especially a fragile and sensitive peptide like insulin that shows extremely low bioavailability through the gastro-intestinal (GIT) route. To address this problem, we have designed a novel drug delivery system (DDS) using precipitation-induced Barium (Ba) salt particles. The DDS can load insulin molecules and transport them through the GIT route. There were several in vitro simulation tests carried out to prove the efficiency of Ba salt particles as oral delivery candidates. All three Ba salt particles (BaSO4, BaSO3, and BaCO3) showed very good loading of insulin (>70% in all formulations) and a degree of resistance throughout a wide range of pHs from basic to acidic conditions when assessed by spectrophotometry. Particles and insulin-associated particles were morphologically assessed and characterized using FE-SEM and FT-IR. A set of tests were designed and carried out with mucin to predict whether the particles are potentially capable of overcoming one of the barriers for crossing intestinal epithelium. The mucin binding experiment demonstrated 60–100% of mucin adhesion to the three different particles. FT-IR identifies the characteristic peaks for mucin protein, particles, and particle-mucin complex re-confirming mucin adhesion to the particles. Finally, the effectiveness of nano-insulin was tested on streptozotocin (STZ) induced diabetic rats. A short acting human insulin analog, insulin aspart, was loaded into Ba salt particles at a dose of 100 IU/Kg prior to oral administration. Among the three formulations, insulin aspart-loaded BaSO4 and BaCO3 particles dramatically reduced the existing hyperglycemia. BaSO4 with loaded Insulin showed an onset of glucose-lowering action within 1 hr, with blood glucose level measured significantly lower compared to the 2nd and 3rd h (p < 0.05). Insulin-loaded BaCO3 particles showed a significant decrease in blood glucose level at 1–2 h, although the glucose level started to show a slight rise at 3rd h and by 4th h, it was back to baseline level. However, although BaSO3 particles with loaded insulin showed a trend of reduction in blood glucose level, the reduction was not found to be significant (p < 0.05) at any point in time. Therefore, oral formulations of insulin/BaSO4 and insulin/BaCO3 particles were observed as effective as native insulin aspart subcutaneous formulation in terms of onset and duration of action. Further investigation will be needed to reveal bioavailability and mechanism of action of this novel Nano-Insulin formulations.

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