Formulation and characterization of Liquid Crystalline Hydrogel of Agomelatin: In vitro and Ex vivo evaluation

Ropinirole (RP), is a selective dopamine agonist that is used alone or with other medications to treat the symptoms of Parkinson’s disease (PD). RP has low bioavailability of only about 50% due to the first-pass metabolism, and it requires frequent dosing during oral administration. The objective of the current research was to develop RP loaded solid lipid nanoparticles (RP-SLNs), nanostructured lipid carriers (RP-NLCs), and their corresponding hydrogels (RP-SLN-C and RP-NLC-C) that might improve efficacy in PD treatment. RP nanoparticles were prepared by homogenization aided probe sonication method and optimized based on particle size, polydispersity index (PDI), zeta potential (ZP), assay, entrapment efficiency, and in vitro release studies. Optimized formulations were converted to hydrogel formulations using Carbopol 934 as a gelling polymer and optimized based on rheological and release characteristics. Optimized formulations were further evaluated using differential scanning calorimetry (DSC), powder X-ray diffractometry (PXRD), scanning electron microscopy (SEM), freeze-drying, and stability study at refrigerated and room temperatures. The optimized RP-SLN formulation showed particle size and entrapment efficiency of 213.5±3.8 nm and 77.9±3.1% compared to 190.6±3.7 nm and 85.7±1.7% for optimized RP-NLC formulation. PXRD supplemented and confirmed DSC results, RP was entrapped in a molecularly dispersed state inside the core of the lipid nanocarrier. Furthermore, RP loaded lipid nanocarriers revealed a spherical shape in SEM images. In vitro release studies demonstrated sustained release profiles for RP from SLNs, NLCs, and their hydrogels over 24 h and were stable over three months at 4ºC and 25ºC storage conditions. Keywords: Parkinson’s disease, Ropinirole, Solid lipid nanoparticles, Nanostructured lipid carriers, Hydrogel.

Section: Stability Studiesmentioning

confidence: 99%

Preparation, In Vitro characterization and stability studies of ropinirole lipid nanoparticles enriched hydrogel for treatment of neurodegeneration diseases

Samanthula¹,

Alli²,

Gorre³

2021

“…They are formed from polymers that are hydrated in an aqueous environment and entrap drug molecules for slow release by diffusion or erosion. The advantages of these buccal hydrogels include extended retention time in the oral cavity, adequate drug penetration, high efficacy and patient acceptability 86,87 . Major application is a medicinal agent for the treatment of periodontitis, which is an inflammatory and infectious disease that causes formation of pockets between the gum and the tooth and leads to loss of teeth 88 .…”

Section: Buccal Hydrogelsmentioning

confidence: 99%

Bioadhesive polymers, permeation enhancers and types of dosage forms for buccal drug delivery

Samanthula¹,

Satla

Bairi³

2021

The buccal delivery is defined as the drug administration through the mucosal membranes lining the cheeks (buccal mucosa). The main impediment to the use of many hydrophilic macromolecular drugs as potential therapeutic agents is their inadequate and erratic oral absorption. Based on our current understanding of biochemical and physiological aspects of absorption and metabolism of many biotechnologically produced drugs, they cannot be delivered effectively through the conventional oral route. Because after oral administration many drugs are subjected to pre-systemic clearance extensive in the liver, which often leads to a lack of significant correlation between membrane permeability, absorption and bioavailability. Difficulties associated with the parenteral delivery and poor oral bioavailability provided the impetus for exploring alternative routes for the delivery of such drugs. This review covers the advantages, disadvantages of buccal delivery, drug and excipient selection especially bioadhesive polymers and permeation enhancers, and further a list of drugs developed as various dosage forms for buccal route of administration. Keywords: Buccal delivery, bioadhesive/mucoadhesive, permeation enhancer, dosage forms.

“…Innovative formulation platforms and tactics for novel oral drug delivery technologies are rapidly being developed to address this issue and increase therapeutic efficacy and safety 5,6 . The range of nano-systems in the oral drug delivery area includes liposomes 7,8 , solid lipid nanoparticles 9,10 , nanocrystals [11][12][13] , liposomes 8,14 , polymeric nanoparticles [15][16][17] which are obtained via specialized techniques such as high pressure homogenizer (HPH) 18,19 . Typically, nano-systems exhibits stability issues caused by agglomeration 20 .…”

Section: Introductionmentioning

confidence: 99%

A Review on Hot Melt Extrusion Coupled Novel Drug Delivery Systems

Parvathaneni¹,

Battu

Sudhakar

2022

The utilization of hot melt extrusion (HME) technology for new applications is increasing in recent years, as evidenced by the many published reports in the last five years. Because of its process automation and low-cost scale-up qualities, which decrease labor expenses and capital investment. HME has emerged as an essential technology for drug delivery applications in pharmaceutical research and manufacture. The novel application of the HME process provides a promising alternate approach in the formulation of novel drug delivery systems. The present review discusses the importance of HME in the development of novel drug delivery systems with the review of relevant case studies. Keywords: hot melt extrusion, novel drug delivery, pharmaceutical research