scholarly journals Clozapine-Encapsulated Binary Mixed Micelles in Thermosensitive Sol–Gels for Intranasal Administration

Gels ◽  
2022 ◽  
Vol 8 (1) ◽  
pp. 38
Author(s):  
Madeleine S. A. Tan ◽  
Preeti Pandey ◽  
James R. Falconer ◽  
Dan J. Siskind ◽  
Alexandra Balmanno ◽  
...  
Keyword(s):  
Intranasal Administration ◽  
Mixed Micelles ◽  
Hydroxypropyl Methylcellulose ◽  
Particle Diameter ◽  
Poloxamer 407 ◽  
Carrier System ◽  
Drug Deposition ◽  
Polysorbate 20 ◽  
Release Studies ◽  
Amorphous Drug

(1) Background: Clozapine is the most effective antipsychotic. It is, however, associated with many adverse drug reactions. Nose-to-brain (N2B) delivery offers a promising approach. This study aims to develop clozapine-encapsulated thermosensitive sol–gels for N2B delivery. (2) Methods: Poloxamer 407 and hydroxypropyl methylcellulose were mixed and hydrated with water. Glycerin and carbopol solutions were added to the mixture and stirred overnight at 2–8 °C. Clozapine 0.1% w/w was stirred with polysorbate 20 (PS20) or polysorbate 80 (PS80) at RT (25 °C) before being added to the polymer solution. The final formulation was made to 10 g with water, stirred overnight at 2–8 °C and then adjusted to pH 5.5. (3) Results: Formulations F3 (3% PS20) and F4 (3% PS80) were selected for further evaluation, as their gelation temperatures were near 28 °C. The hydrodynamic particle diameter of clozapine was 18.7 ± 0.2 nm in F3 and 20.0 ± 0.4 nm in F4. The results show a crystallinity change in clozapine to amorphous. Drug release studies showed a 59.1 ± 3.0% (F3) and 53.1 ± 2.7% (F4) clozapine release after 72 h. Clozapine permeated after 8 h was 20.8 ± 3.0% (F3) and 17.8 ± 3.1% (F4). The drug deposition was higher with F4 (144.8 ± 1.4 µg/g) than F3 (110.7 ± 2.7 µg/g). Both sol–gels showed no phase separation after 3 months. (4) Conclusions: Binary PS80-P407 mixed micelles were more thermodynamically stable and rigid due to the higher synergism of both surfactants. However, binary mixed PS20-P407 micelles showed better drug permeation across the nasal mucosa tissue and may be a preferable carrier system for the intranasal administration of clozapine.

Synthesis, characterization and drug release studies of poly(2-hydroxyethyl methacrylate)/KIT-5 nanocomposite as an innovative organic–inorganic hybrid carrier system

RSC Advances ◽  
2015 ◽  
Vol 5 (16) ◽  
pp. 12463-12471 ◽  
Author(s):  
Roozbeh Javad Kalbasi ◽  
Ali Zirakbash
Keyword(s):  
Controlled Release ◽  
Drug Release ◽  
Hybrid Material ◽  
Great Promise ◽  
Hydroxyethyl Methacrylate ◽  
Carrier System ◽  
Inorganic Hybrid ◽  
Drug Molecules ◽  
System P ◽  
Release Studies

PHEMA/KIT-5 with various pore sizes was prepared. Efficient encapsulation of drug molecules inside the pores of the hybrid material and controlled release of them in an aqueous medium, suggest the great promise of the composite as a carrier system.

FORMULATION DEVELOPMENT AND EVALUATION OF AN IN SITU OPHTHALMIC GELLING SYSTEM OF BRIMONIDINE TARTRATE AND TIMOLOL MALEATE FOR THE TREATMENT OF GLAUCOMA

INDIAN DRUGS ◽  
2017 ◽  
Vol 54 (02) ◽  
pp. 76-78
Author(s):  
A Shirodker ◽  
◽  
S. Bhangle ◽  
R. Gude
Keyword(s):  
Hydroxypropyl Methylcellulose ◽  
In Vitro Release ◽  
Content Uniformity ◽  
Formulation Development ◽  
Timolol Maleate ◽  
Release Studies ◽  
Brimonidine Tartrate ◽  
In Situ Gelling

The present study involved formulation of an in situ gelling system of brimonidine tartrate and timolol maleate for the treatment of glaucoma. Carbopol® 980 NF, xanthum gum and hydroxypropyl methylcellulose K4 M were used as polymers. The prepared in situ gelling systems were evaluated for clarity, appearance, texture analysis, pH, viscosity, rheological properties, in vitro gelation, isotonicity, drug content uniformity, in vitro release studies, microbiological evaluation, ex vivo release studies and stability testing. The results of the attenuated total reflectance spectroscopy and differential scanning calorimetry studies confirmed that there is no incompatibility between the drugs and the excipients. The formulations exhibited pseudoplastic rheology and formulation 3 showed the highest release of both the drugs from the formulation. The stability studies showed that the formulation was stable over the given period of time. Thus, it is evident that the in situ gelling system is a promising drug delivery system for the treatment of glaucoma.

scholarly journals Carrageenan-Based Acyclovir Mucoadhesive Vaginal Tablets for Prevention of Genital Herpes

Marine Drugs ◽  
2020 ◽  
Vol 18 (5) ◽  
pp. 249 ◽  
Author(s):  
Edisson-Mauricio Pacheco-Quito ◽  
Roberto Ruiz-Caro ◽  
Juan Rubio ◽  
Aitana Tamayo ◽  
María-Dolores Veiga
Keyword(s):  
Controlled Release ◽  
Genital Herpes ◽  
Hydroxypropyl Methylcellulose ◽  
Vaginal Fluid ◽  
Vaginal Microbicides ◽  
Safe Method ◽  
Sexually Transmitted ◽  
Vaginal Administration ◽  
Release Studies ◽  
Effective Medication

Women are the most affected by genital herpes, which is one of the most common sexually transmitted infections, affecting more than 400 million people worldwide. The application of vaginal microbicides could provide a safe method of protection. Acyclovir is a safe and effective medication for vaginal administration, and numerous benefits have been observed in the treatment of primary or recurrent lesions due to genital herpes. Vaginal tablets based on a combination of the polymers iota-carrageenan and hydroxypropyl methylcellulose were developed for the controlled release of acyclovir. Swelling, mucoadhesion and drug release studies were carried out in simulated vaginal fluid. The tablets, containing a combination of iota-carrageenan and hydroxypropyl methylcellulose, have an adequate uptake of the medium that allows them to develop the precise consistency and volume of gel for the controlled release of acyclovir. Its high mucoadhesive capacity also allows the formulation to remain in the vaginal area long enough to ensure the complete release of acyclovir. These promising formulations for the prevention of genital herpes deserve further evaluation.

scholarly journals INTRANASAL DELIVERY OF ARTEMETHER FOR THE TREATMENT OF CEREBRAL MALARIA

2018 ◽  
Vol 10 (9) ◽  
pp. 9
Author(s):  
Suman Ramteke ◽  
Roshni Ubnare ◽  
Naveneet Dubey ◽  
Anjita Singh
Keyword(s):  
Plasma Concentration ◽  
Drug Release ◽  
Zeta Potential ◽  
Cerebral Malaria ◽  
Solid Lipid Nanoparticles ◽  
Intranasal Administration ◽  
Lipid Nanoparticles ◽  
Poloxamer 407 ◽  
Solid Lipid ◽  
The Brain

Objective: Nasal delivery provides a route of entry of drug to the brain that circumvents the obstacle for blood-brain barrier allowing direct drug delivery to the central nervous system via olfactory neurons. The objective of work was to prepare solid lipid nanoparticles of antimalarial drug artemether for brain delivery through olfactory delivery route for treatment of cerebral malaria.Methods: Artemether containing solid lipid nanoparticles were prepared with soya lecithin and poloxamer 407 with a hot homogenization method followed by solvent injection technique. The prepared solid lipid nanoparticles were characterized by their shape, particle size, zeta potential, encapsulation efficiency total drug content and drug release study.Results: These solid lipid nanoparticles were observed spherical in shape in scanning electron microscopy, the optimized size was found to be 211.6 nm (Polydispersity Index PI<0.415), with −27mV zeta potential value. The maximum % yield of the formulation was found to be found 49%. The maximum entrapment efficiency was 82% (w/w), and optimized formulation showed 98.07±1.521% drug release form formulation. In vivo studied were conducted on wistar rats after administration of artemether containing solid lipid nanoparticles intranasally and compared with plain artemether solution administered orally. The results of optimized formulation showed the value of biological half-life (T1/2) was 4.95 h, maximum serum concentration Cmax was 644.60ng/ml, time for drug to reach peak plasma concentration Tmax was 1 h volume of distribution (Vd) was 2.7l/kg, body clearance (Cl) was 0.37 lh/kg and Area under curve [AUC]0∞ was 3970.5 nghr/ml for formulation.Conclusion: The results revealed that the brain: plasma concentration ratio was higher after intranasal administration of solid lipid nanoparticles (SLNs) of artemether than the oral route. In conclusion, the intranasal administration of lipid nanoparticles of artemether could provide complete protection against cerebral malaria.

Poloxamer 407/TPGS Mixed Micelles as Promising Carriers for Cyclosporine Ocular Delivery

2018 ◽  
Vol 15 (2) ◽  
pp. 571-584 ◽  
Author(s):  
Maria A. Grimaudo ◽  
Silvia Pescina ◽  
Cristina Padula ◽  
Patrizia Santi ◽  
Angel Concheiro ◽  
...  
Keyword(s):  
Mixed Micelles ◽  
Poloxamer 407 ◽  
Ocular Delivery

scholarly journals Development and Characterization ofIn SituOral Gel of Spiramycin

2014 ◽  
Vol 2014 ◽  
pp. 1-7 ◽  
Author(s):  
Avinash Sharma ◽  
Jyoti Sharma ◽  
Rupinder Kaur ◽  
Vinay Saini
Keyword(s):  
Drug Release ◽  
Sodium Alginate ◽  
High Performance ◽  
Hydroxypropyl Methylcellulose ◽  
Tem Analysis ◽  
Drug Molecules ◽  
Antimicrobial Studies ◽  
Release Studies ◽  
Preformulation Studies

The present investigation deals with the optimization, formulation, and characterization of oralin situgel of spiramycin. Sodium alginate and hydroxypropyl methylcellulose were used as cross-linking and viscosifying agents, respectively. Sodium bicarbonate was used as a floating agent. In preformulation studies, the melting point, pH, and partition coefficient were found to be 133°C, 9.5, and 0.193, respectively. The drug had retention time at around 2.65 minutes in high performance liquid chromatography (HPLC). During compatibility studies of drug with all polymers, we observed that there were no changes in the FTIR spectra of a mixture of drug and polymers. All the formulations showed good pourability. Floating time and total floating time were~30 sec and >12 hours, respectively. Duringin vitrodrug release studies, the drug was released from the formulation around 80–100% for 12–16 hrs. In TEM analysis, we found that the drug molecules were well entrapped in the polymer and the drug was released slowly for up to 12 hrs. In these studies, we found that the concentration of sodium alginate and HPMC had significant influence on floating lag time, gelling capacity, and cumulative percentage drug release. During antimicrobial studies, we found that the formulation containing spiramycin showed good zone of inhibition against different microbial strains (Staphylococcus aureusandEscherichia coli).

scholarly journals Characteristic Evaluation of Gel Formulation Containing Niosomes of Melatonin or Its Derivative and Mucoadhesive Properties Using ATR-FTIR Spectroscopy

Polymers ◽  
2021 ◽  
Vol 13 (7) ◽  
pp. 1142
Author(s):  
Prangtip Uthaiwat ◽  
Aroonsri Priprem ◽  
Ploenthip Puthongking ◽  
Jureerut Daduang ◽  
Chatchanok Nukulkit ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Ftir Spectroscopy ◽  
Oral Drug Delivery ◽  
Hydroxypropyl Methylcellulose ◽  
Poloxamer 407 ◽  
Oral Drug ◽  
Attenuated Total Reflectance ◽  
Total Reflectance ◽  
Gelling Agents ◽  
Mucoadhesive Property

Chitosan or polyvinyl pyrrolidone (PVP) were used in combination with hydroxypropyl methylcellulose (HPMC) and poloxamer 407 (P407) as gelling agents for oral drug delivery. The performance interaction with mucin of chitosan-composed gel (F1) and PVP-composed gel (F2) was compared using attenuated total reflectance–Fourier-transform infrared (ATR-FTIR) spectroscopy at controlled temperatures of 25 and 37 °C for 1 and 5 min. F1 containing niosome-entrapped melatonin or its derivatives was investigated for mucoadhesive interaction on mucosa by ATR-FTIR spectroscopy under the same conditions. The results showed that F1-treated mucin gave a significantly lower amide I/amide II ratio than untreated mucin and F2-treated mucin did within 1 min, suggesting improved rapid affinity between mucin and chitosan. The spectra of mucosa treated with F1 incorporating niosomes of melatonin or its derivatives showed peak shifts at C=O (amide I), N-H (amide II), and carbohydrate regions and an associated decrease in the amide I/amide II ratio and increase in the carbohydrate/amide II ratio. These results indicated electrostatic interaction and hydrogen bonding between chitosan and mucin on the mucosa. In conclusion, the molecular interaction between gels and mucin/mucosa detected at amide I and amide II of proteins and the carbohydrate region could lead to an improved mucoadhesive property of the gel on the mucosa.

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