Intranasal RepaglinideSolid lipid nanoparticles integrated in situ gel outperform conventional oral route in hypoglycemic activity

Author(s):  
Soha M. ELkarray ◽  
Ragwa M. Farid ◽  
Mohammad M. Abd-Alhaseeb ◽  
Gamal A. Omran ◽  
Doaa A. Habib
Nanomaterials ◽  
2018 ◽  
Vol 9 (1) ◽  
pp. 33 ◽  
Author(s):  
Akshaya Tatke ◽  
Narendar Dudhipala ◽  
Karthik Janga ◽  
Sai Balguri ◽  
Bharathi Avula ◽  
...  

Triamcinolone acetonide (TA), an intermediate acting corticosteroid, is used in the treatment of posterior ocular diseases, such as inflammation, posterior uveitis, and diabetic macular edema. The objective of this investigation was to prepare TA-loaded solid lipid nanoparticles (TA-SLNs) and in situ gel (TA-SLN-IG) formulations for delivery into the deeper ocular tissues through the topical route. TA-SLNs were prepared by hot homogenization and ultrasonication method using glyceryl monostearate and Compritol® 888ATO as solid lipids and Tween®80 and Pluronic® F-68 as surfactants. TA-SLNs were optimized and converted to TA-SLN-IG by the inclusion of gellan gum and evaluated for their rheological properties. In vitro transcorneal permeability and in vivo ocular distribution of the TA-SLNs and TA-SLN-IG were studied using isolated rabbit corneas and New Zealand albino rabbits, respectively, and compared with TA suspension, used as control (TA-C). Particle size, PDI, zeta potential, assay, and entrapment efficiency of TA-SLNs were in the range of 200–350 nm, 0.3–0.45, −52.31 to −64.35 mV, 70–98%, and 97–99%, respectively. TA-SLN-IG with 0.3% gellan gum exhibited better rheological properties. The transcorneal permeability of TA-SLN and TA-SLN-IG was 10.2 and 9.3-folds higher compared to TA-C. TA-SLN-IG showed maximum tear concentration at 2 h, indicating an improved pre-corneal residence time, as well as higher concentrations in aqueous humor, vitreous humor and cornea at 6 h, suggesting sustained delivery of the drug into the anterior and posterior segment ocular tissues, when compared to TA-SLN and TA-C. The results, therefore, demonstrate that the lipid based nanoparticulate system combined with the in situ gelling agents can be a promising drug delivery platform for the deeper ocular tissues.


2016 ◽  
Vol 4 (2) ◽  
pp. 11-19 ◽  
Author(s):  
Pallavi Chand ◽  
Pratibha . ◽  
G. Gnanarajan ◽  
Preeti Kothiyal

Oral route is technique which is used over a decades. It is most preferred and common technique for oral administration of drug in the body, but due to certain limitation such as absorption of drug, drug targeting to particular organ can cause problem for administration through oral route. To overcome these types of problem as well as for improvement of drug safety and efficiency a novel approach is developed for delivery of drug i.e. In-situ Nasal Drug Delivery System. In-situ gel is a process in which sol form before administration in the body, but once administrated, it undergo gelation in-situ, to form gel. Nasal drug delivery is one of alternative viable route of drug delivery is one of alternative and viable route of drug delivery. Nasal route is rich in vasculature and highly permeable. Nasal route is suitable for those drugs whose oral administration is problematic due to gastric irritation. The present review focused on anatomy of nasal system and criteria required of drug candidate to prepare a gel i.e. In-situ gel. Approaches towards various formulation of in-situ gel with respect to temperature, ph and physiochemical condition.The main role of polymers like Poloxamer, Pectine, Cellulose etc in body, absorption of drug by various methods. Various evaluation parameters which is consider during preparation of in-situ gel.


2019 ◽  
Vol 9 (2) ◽  
pp. 442-448 ◽  
Author(s):  
Rabiah Bashir ◽  
Asmat Majeed ◽  
Tabasum Ali ◽  
Saeema Farooq ◽  
Nisar Ahmad Khan

The drugs having a narrow absorption window in the gastrointestinal tract (GIT) when administered by oral route are often limited by poor bioavailability due to incomplete drug release and short residence time at the site of absorption. Novel drug delivery systems in the form of gastroretentive systems such as floating systems, mucoadhesive, high-density, expandable have been developed as they provide controlled delivery of drugs with prolonged gastric residence time. Liquid orals are more prone to low bioavailability because they are eliminated quickly from the stomach since they are subjected to faster transit from the stomach/ duodenum. The problems of immediate release and short gastrointestinal residence of liquids are eliminated by formulating as oral in situ gels as they provide the best means to overcome these problems The in situ gel dosage form is a liquid before administration and after it comes in contact with gastric contents due to one or more mechanisms gets converted to gel which floats on gastric contents. This achieves increased residence as well as sustained release. This approach is useful for systemic as well as local effect of drugs administered. This review gives a brief idea about floating oral in-situ gel formation and research done by various scientists on a number of drugs and polymers. Keywords: Floating drug delivery, gastric retention time, In-situ gel.


2018 ◽  
Vol 548 (1) ◽  
pp. 609-624 ◽  
Author(s):  
Nancy Abdel Hamid Abou Youssef ◽  
Abeer Ahmed Kassem ◽  
Ragwa Mohamed Farid ◽  
Fatma Ahmed Ismail ◽  
Magda Abd Elsamea EL-Massik ◽  
...  

2016 ◽  
Vol 6 (1) ◽  
pp. 56 ◽  
Author(s):  
DineshKumar Pandurangan ◽  
Prathima Bodagala ◽  
VijayarajKumar Palanirajan ◽  
Saravanan Govindaraj

Author(s):  
Anuradha P Prajapati ◽  
Jalpa H Kanzaria ◽  
Shailesh V Luhar ◽  
Sachin B Narkhede

The objective of the present work is to formulate, develop and evaluate nasal in situ gel of Pregabalin to provide better therapy for Epilepsy. Pregabalin is BCS class I drug. It is 3rd generation anticonvulsant used in epilepsy in which faster action is required. Nasal route has faster action than oral route, also convenient to unconscious patient. Pregabalin loaded in situ gel, for the treatment of epilepsy to avoid side effects and first pass metabolism associated with conventional treatment and increase bioavailability. Pregabalin was loaded into different polymeric solutions of Polycarbophil and HPMC K4M. The drug was characterized for various parameters like UV-Spectroscopy, FTIR Spectroscopy and DSC study. Excipients were screened for selection of mucoadhesive and gelling polymer. Then the drug was formulated as in situ gel. The experiment was subjected to 32 full factorial design, the concentration of Polycarbophil (X1) and HPMC K4M (X2) were selected as independent variables with % drug release and muco-adhesive strength as dependent variables. The kinetic study was carried out for 30 days. Polycarbophil was selected as mucoadhesive and gelling polymer. The values for X1 and X2 were 0.3922% and 0.5263% relating the % drug release and mucoadhesive strength values were 78.20% CDR at 240 min. and 960 dynes/cm2 respectively for checkpoint batch following zero order and Higuchi kinetic. The formulation was found to be stable for 30 days. The present research will be helpful in order to improve the efficacy and tolerability of the antiepileptic drug therapy. So alternative administration strategy has been investigated which deliver nasally administered medication directly to brain effectively. The intranasal in situ gelling system is a promising novel drug delivery system for an antiepileptic drug Pregabalin which could enhance nasal residence time with increased viscosity and mucoadhesive character and provided better release profile of drug for treating epileptic conditions.  


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