Formulation Development of Nifedipine through Nanotechnology: A Comprehensive Review

2021 ◽  
Vol 09 ◽  
Author(s):  
Sabarni Sarker ◽  
Md. Rajdoula Rafe
Keyword(s):  
Channel Blocker ◽  
Polymeric Nanoparticles ◽  
Rapid Onset ◽  
Lipid Nanoparticles ◽  
Water Soluble ◽  
Technological Innovations ◽  
Formulation Development ◽  
Solubility Profile ◽  
Pharmacokinetic Properties ◽  
Dihydropyridine Calcium Channel Blocker

Background: The therapeutic use of nifedipine, a dihydropyridine calcium channel blocker, is limited due to its poor solubility profile, rapid onset of its action, and short biological half-life. Many formulation techniques have been applied to improve the properties of the drug. Objective: The objective of the study is to summarize the nanotechnology approaches designed to improve the therapeutic and pharmacokinetic properties of nifedipine till 2020. Methods: The related articles were searched until 28th March, 2020, with the specific keywords, in Pubmed and google scholar, excluding review articles. Results: The discussion showed that among the nano-carriers used to improve the pharmacological property of the drug, lipid nanoparticles, polymeric nanoparticles, crystalline nanoparticles, and nano-emulsions have been used widely. Nanotechnology has been found efficient in improving the solubility profile of nifedipine, achieving sustained and controlled release, and achieving targeted and local delivery and transdermal drug delivery. By exploiting nano-formulations, new windows of therapeutic applications can be achieved. Furthermore, micelle media, polymeric nanoparticles, and microcrystalline nanoparticles have been used to develop a photostable formulation. Conclusion: The technological innovations in the field of nanomedicine have paved many ways for delivering nifedipine and such sparingly water-soluble compounds.

scholarly journals Formulation and Characterization of Nimodipine Nanoparticles for the Enhancement of solubility and dissolution rate

2021 ◽  
Vol 30 (2) ◽  
pp. 143-152
Author(s):  
Areej Wahhab Alhagiesa ◽  
Mowafaq M. Ghareeb
Keyword(s):  
Particle Size ◽  
Dissolution Rate ◽  
Channel Blocker ◽  
Polymeric Nanoparticles ◽  
Poloxamer 407 ◽  
High Permeability ◽  
Freeze Dried ◽  
Dihydropyridine Calcium Channel Blocker ◽  
Low Solubility

Nimodipine (NMD) is a dihydropyridine calcium channel blocker useful for the prevention and treatment of delayed ischemic effects. It belongs to class ? drugs, which is characterized by low solubility and high permeability. This research aimed to prepare Nimodipine nanoparticles (NMD NPs) for the enhancement of solubility and dissolution rate. The formulation of nanoparticles was done by the solvent anti-solvent technique using either magnetic stirrer or bath sonicator for maintaining the motion of the antisolvent phase. Five different stabilizers were used to prepare NMD NPs( TPGS, Soluplus®, HPMC E5, PVP K90, and poloxamer 407). The selected formula F2, in which  Soluplus  has been utilized as a stabilizer, has a particle size (77 nm) and polydispersity index (PDI) (0.016). The formulas with the smallest particle size were freeze dried with the addition of 1 % w/w mannitol as cryoprotectant. The saturation solubility of NMD in the prepared nanoparticles was increased twenty four-folds, and the complete dissolution was achieved at 90 minutes compared with pure NMD, which reaches only 6%. The formation of hydrogen bonding between NMD and the polymer or the cryoprotectant, as confirmed by the FTIR study. In conclusion, the preparation of NMD as polymeric nanoparticles is a useful technique for enhancing the solubility and dissolution rate.

scholarly journals FORMULATION AND EVALUATION OF NANOPARTICLES WITH NEURO PROTECTIVE CHEMICALS OF NATURAL AND SYNTHETIC ORIGIN.

2021 ◽  
pp. 11-14
Author(s):  
Pallav Kaushik Deshpande ◽  
Ragini Gothalwal
Keyword(s):  
Drug Delivery ◽  
Polymeric Nanoparticles ◽  
Drug Loading ◽  
Ethanolic Extract ◽  
Lipid Nanoparticles ◽  
Water Soluble ◽  
Drug Release Profile ◽  
Standard Drug ◽  
Conventional Drug ◽  
Nanoparticle Design

Most of the active phytoconstituents under development are poorly water soluble or have poor bioavailability . Nanotechnology is an approach to overcome the challenges of conventional drug delivery systems and limitations of phytochemicals. Solid Lipid nanoparticles show interesting features concerning therapeutic purposes. The main advantage is that they are prepared with physiologically well-tolerated lipids.Solid Lipid Nanoparticles (SLNs) as novel lipid based nanocarriers with size range between 10 to 1000nm. SLNs were introduced to overcome problems of polymeric nanoparticles.In present research formulation and evaluation of nanoparticles with ethanolic extract of two plants Celastrus paniculatus and Bacopa monnieri along with Donepezil as a standard drug was undertaken here for the production methods for preparation of SLNs, and pharmaceutical approach of SLNs in drug delivery . The focus of nanoparticle design over the years has evolved toward more complex nanoscopic core–shell architecture using a single delivery system to combine multiple functionalities within nanoparticles which combine the mechanical advantages of biodegradable polymeric nanoparticles and biomimetic advantages of liposomes, have emerged as a robust and promising delivery platform. Solid liquid nanoparticles having plant extracts were successfully formulated and characterized for their stability.A biodegradable polymeric core is surrounded by a shell composed of layer(s) of phospholipids. This architecture can provide advantages such as controllable particle size, surface functionality, high drug loading, entrapment of multiple therapeutic agents, drug release profile,and good serum stability of phytochemicals

Formulation Development of Tamoxifen Loaded Lipid Nanoparticle by Taguchi (L12 (2 11)) Orthogonal Array Design

2020 ◽  
Vol 16 ◽  
Author(s):  
Poovi Ganesan ◽  
N Damodharan
Keyword(s):  
Orthogonal Array ◽  
Drug Loading ◽  
Optimization Technique ◽  
Pharmaceutical Products ◽  
Water Soluble ◽  
Nanostructured Lipid Carrier ◽  
Orthogonal Array Design ◽  
Formulation Development ◽  
Array Design ◽  
Lipid Nanoparticle

Background: A better understanding of the biopharmaceutical and physicochemical properties of drugs and the pharmaco-technical factors would be of great help for developing pharmaceutical products. But, it is extremely difficult to study the effect of each variable and interaction among them through the conventional approach Objective: To screen the most influential factors affecting the particle size (PS) of lipid nanoparticle (LNPs) (solid lipid nanoparticle (SLN) and nanostructured lipid carrier (NLC)) for poorly water-soluble BCS class-II drug like tamoxifen (TMX) to improve its oral bioavailability and to reduce its toxicity to tolerable limits using Taguchi (L12 (2 11)) orthogonal array design by applying computer optimization technique. Results: The size of all LNPs formulations prepared as per the experimental design varied between 172 nm and 3880 μm, polydispersity index between 0.033 and 1.00, encapsulation efficiency between 70.8% and 75.7%, and drug loading between 5.84% and 9.68%. The study showed spherical and non-spherical as well as aggregated and non-aggregated LNPs. Besides, it showed no interaction and amorphous form of the drug in LNPs formulation. The Blank NLCs exhibited no cytotoxicity on MCF-7 cells as compared to TMX solution, SLNs (F5) and NLCs (F12) suggests that the cause of cell death is primarily from the effect of TMX present in NLCs. Conclusions: The screening study clearly showed the importance of different individual factors significant effect for the LNPs formulation development and its overall performance in an in-vitro study with minimum experimentation thus saving considerable time, efforts, and resources for further in-depth study.

Optimization of Solid Lipid Nanoparticles of Ezetimibe in Combination with Simvastatin Using Quality by Design (QbD)

2020 ◽  
Vol 10 (4) ◽  
pp. 404-418
Author(s):  
Kruti Borderwala ◽  
Ganesh Swain ◽  
Namrata Mange ◽  
Jaimini Gandhi ◽  
Manisha Lalan ◽  
...  
Keyword(s):  
Particle Size ◽  
Solid Lipid Nanoparticles ◽  
High Speed ◽  
Entrapment Efficiency ◽  
Lipid Nanoparticles ◽  
Water Soluble ◽  
Lipid Matrix ◽  
Solid Lipid ◽  
32 Factorial Design ◽  
Full Factorial Experimental Design

Background: The objective of this study was to develop solid lipid nanoparticles (SLNs) of poorly water soluble anti-hyperlipidemic drugs-Ezetimibe in combination with Simvastatin. Methods: This study describes a 32 full factorial experimental design to optimize the formulation of drug loaded lipid nanoparticles (SLN) by the high speed homogenization technique. The independent variables amount of lipid (GMS) and amount of surfactant (Poloxamer 188) were studied at three levels and arranged in a 32 factorial design to study the influence on the response variables- particle size, % entrapment efficiency (%EE) and cumulative drug release (% CDR) at 24 h. Results: The particle size, % EE and % CDR at 24 h for the 9 batches (B1 to B9) showed a wide variation of 104.6-496.6 nm, 47.80-82.05% (Simvastatin); 48.60-84.23% (Ezetimibe) and 54.64-92.27% (Simvastatin); 43.8-97.1% (Ezetimibe), respectively. The responses of the design were analysed using Design Expert 10.0.2. (Stat-Ease, Inc, USA), and the analytical tools of software were used to draw response surface plots. From the statistical analysis of data, polynomial equations were generated. Optimized formulation showed particle size of 169.5 nm, % EE of 75.43% (Simvastatin); 79.10% (Ezetimibe) and 74.13% (Simvastatin); 77.11% (Ezetimibe) %CDR after 24 h. Thermal analysis of prepared solid lipid nanoparticles gave indication of solubilisation of drugs within lipid matrix. Conclusion: Fourier Transformation Infrared Spectroscopy (FTIR) showed the absence of new bands for loaded solid lipid nanoparticles indicating no interaction between drugs and lipid matrix and being only dissolved in it. Electron microscope of transmission techniques indicated sphere form of prepared solid lipid nanoparticles with smooth surface with size approximately around 100 nm.

scholarly journals REVIEW ARTICLE: SOLUBILITY ENHANCEMENT BY SOLID DISPERSION

2017 ◽  
Vol 9 (3) ◽  
pp. 15
Author(s):  
A. N. Patil ◽  
D. M. Shinkar ◽  
R. B. Saudagar
Keyword(s):  
Solid Dispersion ◽  
Aqueous Solubility ◽  
Water Soluble ◽  
Full Potential ◽  
Drug Selection ◽  
Formulation Development ◽  
Poorly Water Soluble Drugs ◽  
New Chemical Entities ◽  
Water Soluble Drugs ◽  
Poorly Water Soluble

Enhancement of solubility, dissolution rate and bioavailability of the drug is a very challenging task in drug development, nearly 40% of the new chemical entities currently being discovered are poorly water soluble drugs. The solubility behaviour of the drugs remains one of the most challenging aspects in formulation development. This results in important products not reaching the market or not achieving their full potential. Solid dispersion is one of the techniques adopted for the formulation of such drugs and various methods are used for the preparation of solid dispersion. Solid dispersion is generally prepared with a drug which is having poor aqueous solubility and hydrophilic carrier. This article review various methods and concept of solid dispersion, criteria for drug selection, advantage and disadvantage, characterization, and application.

scholarly journals Non-Traditional Administration of Remifentanil in an Experimental Setting

2019 ◽  
pp. S97-S103
Author(s):  
A. KURZOVÁ ◽  
J. MÁLEK ◽  
L. HESS ◽  
M. JAČEK ◽  
J. SLÍVA
Keyword(s):  
Arterial Oxygen Saturation ◽  
Pharmacokinetic Profile ◽  
Rapid Onset ◽  
Arterial Oxygen ◽  
Onset Of Action ◽  
Routes Of Administration ◽  
Arterial Blood ◽  
Pharmacokinetic Properties ◽  
Righting Reflex ◽  
Cardiovascular Functions

Remifentanil is ultrashort-acting opioid with a unique pharmacokinetic profile. It is used exclusively intravenously. While considering its rapid onset of action and other pharmacokinetic properties, we decided to assess its effects following administration via non-traditional routes. Rabbits (n=10 per each group) were randomized into six groups: remifentanil 1 μg/kg and 3 μg/kg IM, 5.0 and 10.0 μg/kg conjunctivally, and 10 μg/kg and 25.0 μg/kg intranasally. Sedating effects were assessed via a loss of the righting reflex. Secondary, mean arterial blood pressure, arterial oxygen saturation of hemoglobin, and pulse rate was monitored in all rabbits. Non-traditional routes of administration were shown to provide a rapid onset of action as well as fast recovery. Importantly, the administration of remifentanil did not result in any deterioration of cardiovascular functions.

scholarly journals Unresponsive shock due to amlodipine overdose: An unexpected cause

2018 ◽  
Vol 10 (4) ◽  
pp. 246-247 ◽  
Author(s):  
Shailesh Kumar ◽  
Devyani Thakur ◽  
Ritesh Kumar Gupta ◽  
Alka Sharma
Keyword(s):  
Channel Blocker ◽  
Kidney Injury ◽  
Poor Performance ◽  
Interesting Case ◽  
Young Lady ◽  
Fluid Replacement ◽  
Refractory Shock ◽  
Shock Reversal ◽  
Dihydropyridine Calcium Channel Blocker ◽  
Hypertensive Drug

Amlodipine is a dihydropyridine calcium channel blocker which is widely used as an anti-hypertensive drug. Amlodipine overdose has been infrequently reported with the occurrence of serious complications and even death in a few cases. We report an interesting case of a young lady who presented with refractory shock with acute kidney injury, which did not respond to therapy despite optimal fluid replacement and vasopressor support. The etiology of shock could not be ascertained and the patient was questioned again to elucidate the missing clue in the history. It was finally revealed that the patient had consumed 900 mg of amlodipine in a suicide bid, for her poor performance in academics. The targeted therapy in the form of IV calcium and hyperinsulinemia-euglycemia therapy (HIET) was started and the patient dramatically improved with shock reversal and improvement in renal function.

scholarly journals Effect of Dihydropyridine Calcium-Channel Blocker on Adverse Aortic Events After Thoracic Endovascular Aortic Repair for Type B Aortic Dissection

2021 ◽  
Author(s):  
Fan Yang ◽  
Lyufan Chen ◽  
Jitao Liu ◽  
Songyuan Luo ◽  
Caiyun He ◽  
...  
Keyword(s):  
Propensity Score ◽  
Aortic Dissection ◽  
Calcium Channel ◽  
Propensity Score Matching ◽  
Calcium Channel Blocker ◽  
Channel Blocker ◽  
Thoracic Endovascular Aortic Repair ◽  
Type B ◽  
Type B Aortic Dissection ◽  
Dihydropyridine Calcium Channel Blocker

Abstract Objectives: This study aimed to evaluate the effect of dihydropyridine calcium-channel blocker (CCB) on adverse aortic events (AAE) in patients undergoing thoracic endovascular aortic repair (TEVAR) for type B aortic dissection (TBAD). Methods: A retrospective study was conducted on patients undergoing TEVAR of TBAD from January 2010 to December 2017 in our center. Patients were divided into CCB group and non-CCB group according to the postoperative dihydropyridine CCB use. AAE including aorta-relative mortality and reintervention, were compared between these two groups. Propensity score matching analysis was performed to avoid the potential effect of known confounders.Results: Before matching, the study cohort comprised 548 patients, including 435 (79.4%) and 113 (20.6%) patients in the CCB and non-CCB groups, respectively. After matching, 101 patients in each group were eligible for the analysis. In the unmatched cohort, AAE occurred in 52 (12.0%) and 29 (25.7%) patients in the CCB and non-CCB groups, respectively (P < 0.001). In the matched cohort, AAE occurred in 8 (7.9%) and 22 (21.8%) patients in the CCB and non-CCB groups, respectively (P = 0.013). Log-rank test analysis revealed that the levels of freedom from AAE were significantly different between the 2 groups in both the unmatched and matched cohorts (P < 0.001 and P = 0.007, respectively). Multivariable analysis showed that CCB use (hazard ratio 0.50, 95% confidence interval 0.32–0.80; P = 0.003) was associated with a lower AAE rate after adjustment for other variables, and was minimally changed after the propensity score matching (HR 0.34, 95% CI 0.15–0.75; P = 0.008).Conclusions: Postoperative dihydropyridine CCB use is protective in patients undergoing TEVAR for acute and sub-acute TBAD.

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