scholarly journals A Review on New Trends in Preparation of Long Acting Microspheres

2019 ◽  
Vol 9 (5) ◽  
pp. 192-198 ◽  
Author(s):  
Prateek Pathak ◽  
Sarvesh Paliwal

The Purpose of designing sustained or controlled delivery systems has always been to bring down the dose frequency that offers better patient compliance & reduced side effects Microspheres have shown to reduce the dose, side effects, frequency of administration and possibility of dose dumping, therefore increased patient compliance. There are several methods of preparation for microspheres, slight variation in basic method can produce numerous changes in final outcome. However various problems are still not resolved with these methods like wide size distribution & poor repeatability. Biodegradation rate of the microspheres in controlled by the composition of the microspheres and consecutively affects the release profile of drug, i.e. PGA, PLA and PCL have hydrolytic degradation role in order of PGA>PLA>>PCL.     Keywords: controlled delivery, microspheres, patient compliance

1961 ◽  
Vol 38 (1) ◽  
pp. 73-87 ◽  
Author(s):  
Christian Lauritzen ◽  
Semih Velibese

ABSTRACT A description is given of experimental investigations and preliminary clinical experience with the long-acting oestriol compound polyoestriol phosphate – a water-soluble polymere of oestriol and phosphoric acid. The compound seems to exert all the physiologically important effects of oestriol. Even with high doses the hormone causes no proliferation of the endometrium and no withdrawal bleeding. It has no untoward effect on metabolism. It decreases slightly the cholesterol concentration (to the extent of ⅓–⅕ of the effect produced by long-acting oestradiol esters). The compound has a wide therapeutic range. No side-effects have been observed. Doses of 10 mg or more have a prolonged duration. Additional prolongation of the effect is largely dependent on dosage. To ensure an effect lasting for 4 weeks 40 mg polyoestriol phosphate (corresponding with 30 mg oestriol) is required – an amount which roughly corresponds with physiological quantitative data. The compound, which involves an interesting new principle of prolongation, was most effectively used in the treatment of menopausal symptoms and genital organic disorders. For these indications it can be recommended without reservation.


2021 ◽  
Vol 11 (01) ◽  
pp. e199-e204
Author(s):  
Osama Mahmoud El-Asheer ◽  
Ahmed Gaber Ahmed ◽  
Zainab AbdelAal Abdel Hafez ◽  
Marwa AbdelHafiz Dahpy ◽  
Amal AbdElSalam Soliman

AbstractLactoferrin (LF) is an iron-binding globular glycoprotein that is structurally and chemically similar to serum transferrin. Many studies have been done to evaluate the effect of oral LF administration on iron deficiency anemia (IDA) with controversial results. This study was designed to compare the efficacy of LF versus oral ferrous sulfate (OFS) therapy in the treatment of children with IDA. A significant increase in mean hemoglobin and serum iron concentrations was noted in the group that received oral bovine LF (11.06 ± 0.96 and 42.79 ± 6.14, respectively) versus the group that received OFS (10.24 ± 0.57 and 28.94 ± 5.05, respectively, with p < 0.001 for each) after 30 days of the treatment with fewer side effects (9.3 vs. 33.3% with p = 0.043). Oral bovine LF is a more effective and safer alternative in treating iron deficiency and IDA compared with OFS with clinical benefits of fewer side effects and better patient compliance.


Author(s):  
R Segarra ◽  
M Recio-Barbero ◽  
M Sáenz-Herrero ◽  
O Mentxaka ◽  
J Cabezas-Garduño ◽  
...  

Abstract Background Long-acting injectable antipsychotics (LAIs) may be a suitable therapeutic option for those patients in earlier stages of psychosis to avoid relapses and disease progression. Despite that, there is a lack of evidence in the literature regarding the use of LAIs in this profile of patients. Methods This is a retrospective cohort analysis to assess the efficacy, tolerability, and pattern of use of palmitate paliperidone long-acting injectable (PPLAI) formulations (1-monthly and 3-monthly) compared to oral paliperidone/risperidone in patients with a non-affective First Psychotic Episode(FEP) over a 12-month follow-up. Relevant sociodemographic and clinical information were assessed as well as main clinical scales: Positive and Negative Syndrome Scale (PANSS), Personal and Social Performance Scale (PSP), and Clinical Global Impression Scale (CGI-I and CGI-S). Results Forty-eight patients, 16 per arm, 20-50 year aged with a FEP were included. Significant improvements were registered for all treatment groups. Despite that, patients receiving PPLAI 1-monthly and PPLAI 3-monthly formulations obtained greater improvements than the oral group in the main domains assessed (p&lt;0.001). We found no statistically significant differences in hospitalizations between groups. Side effects were presented in 24% of patients. A trend towards reducing antipsychotic doses was observed in 43.8% of patients to achieve the minimum effective dose and avoid the occurrence of side effects. Conclusions To our knowledge, this is the first study assessing the use of palmitate paliperidone long-acting formulations versus oral risperidone or paliperidone in FEP. Treatment with PPLAI formulations seems to be an effective therapeutic choice at earlier stages of the disease.


Polymers ◽  
2018 ◽  
Vol 10 (12) ◽  
pp. 1379 ◽  
Author(s):  
Sarah Stewart ◽  
Juan Domínguez-Robles ◽  
Ryan Donnelly ◽  
Eneko Larrañeta

The oral route is a popular and convenient means of drug delivery. However, despite its advantages, it also has challenges. Many drugs are not suitable for oral delivery due to: first pass metabolism; less than ideal properties; and side-effects of treatment. Additionally, oral delivery relies heavily on patient compliance. Implantable drug delivery devices are an alternative system that can achieve effective delivery with lower drug concentrations, and as a result, minimise side-effects whilst increasing patient compliance. This article gives an overview of classification of these drug delivery devices; the mechanism of drug release; the materials used for manufacture; the various methods of manufacture; and examples of clinical applications of implantable drug delivery devices.


2021 ◽  
Vol 14 (1) ◽  
pp. 11-15
Author(s):  
Łukasz Hajac ◽  
Martyna Hajac ◽  
Adam Maciejczyk

Nausea and vomiting are one of most frequent side effects of chemotherapy and radiotherapy. Effective prevention and treatment of these symptoms is essential for better quality of life for patients undergoing oncological therapies. Nausea and vomiting can be acute, delayed or anticipatory. Leading mechanisms and methods of treatment are different for each of those. Most often used groups of drugs are: 5-HT3-antagonists, glucocorticosteroids, NK1-antagonists. Another important group are neuroleptics, which are therapy of choice for anticipatory vomiting. Modern antiemetic medications are in most cases safe and effective. But as every treatment it causes risks of adverse events which may be serious and difficult to manage. It applies in particular to long-acting drugs. Most common side effects are headache, constipation and sedation. But more severe or life-threatening symptoms may appear, like intestinal obstruction and serotonin syndrome. Some of the drugs also come with risk of interacting with other treatment. Changes in pharmacokinetics may lead to additional toxicities. In elderly, especially with cardiac disease, in risk of ileus or cachexia these drugs shall be used with caution.


Author(s):  
GA. Alcántara Blanco ◽  
N. Urdaneta ◽  
MA. Sabino

In this research two dibenzylideneacetone (DBA) analogs compounds: (1E,4E)-1-(4-(dimethylamino)phenyl)-5-(4-methoxyphenyl)penta-1,4-dien-3-one (DBA-1) and (1E,4E)-1-(4-methoxyphenyl)-5-(4-nitrophenyl)penta-1,4-dien-3-one (DBA-2) were encapsulated in poly(lactic acid) (PLA) membranes. These DBA analogs can have several applications such as in the development of controlled drug release systems and tissue engineering.  The membranes were elaborated by solvent casting. It was found that these fluorescent compounds have a small percentage of hemolysis in human blood red cells at concentrations between 200-500 µg/mL. Therefore, they can be considered not-toxic at these concentrations. The hydrolytic degradation of PLA membranes loaded with the DBA analogs was studied at a temperature of 37 °C under solutions at acid, neutral, and basic pH conditions for a maximum time of six weeks. The hydrolysis was monitored by measuring the loss of mass of the membranes, changes in pH environments, variations in the molecular weight of PLA matrix, and changes in surface morphology observed through Scanning the Electron Microscopy (SEM) technique. Applying UV-visible spectrophotometry, the amount released from the DBA analogs in the PLA membranes was determined during the degradation time, and finally, the release profile was obtained. It was observed employing SEM that the membranes presented a major degradation under basic pH conditions, with a higher percentage of release in an acid medium for both analogues of DBA studied


2009 ◽  
Vol 161 (5) ◽  
pp. 795-798 ◽  
Author(s):  
J W Jacobeit ◽  
L J Gooren ◽  
H M Schulte

DesignTestosterone treatment is essential for the induction and maintenance of virilization of female-to-male (FTM) transsexuals.AimTo test the safety of a novel testosterone preparation for this purpose.MethodsParenteral long-acting testosterone undecanoate (TU) was administered to 17 FTM transsexuals over 36 months. Observations were made while subjects received treatment.ResultsSerum testosterone rose from 0.50±0.25 to 6.2±1.3 ng/ml at 6 months and remained stable thereafter. The testosterone profiles were largely identical with those in hypogonadal receiving TU. There were no side effects. Over the 36 months of the study, there was a small but significant decrease in plasma cholesterol (from 218±47 to 188±42 mg/dl) and low-density lipoprotein-cholesterol (from 139±48 to 139±48 mg/dl), while plasma levels of high-density lipoprotein-cholesterol and triglycerides did not change significantly. Liver enzymes did not change during treatment. There was an increase of both levels in hemoglobin (from 13.6±1.2 to 16.0±1.5 g/dl) and hematocrit (from 41±4 to 46±4) upon administration but they remained almost without exception within the physiological range. No special measures were needed. Breast and gonads/internal genitalia did not show pathological changes over the observation period.ConclusionThis study reports that TU is suited for induction of virilization in FTM transsexuals without significant side effects over a longer term.


Author(s):  
Justin C. Ellison ◽  
Jason B. Rosenstock ◽  
Michael J. Marcsisin

A variety of somatic therapies can be used to treat individuals suffering from psychosis. Most commonly, providers will prescribe antipsychotics, which generally block dopamine receptors and are particularly useful at reducing positive symptoms. Second-generation antipsychotics have fewer movement side effects than older agents do, but they are more expensive and have more metabolic side effects. Long-acting injectable (LAI) antipsychotics can be useful for improving outcomes, especially in non-adherent patients, and clozapine is the gold standard for treatment-refractory psychosis. Other agents may be useful for adjunct therapy, or in early psychosis, such as antidepressants, mood stabilizers, and benzodiazepines. In this chapter, we will also review other somatic therapies such as electroconvulsive therapy (ECT) and other neuromodulation approaches.


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