Controlled bimatoprost release from graphene oxide laden contact lenses: In vitro and in vivo studies
Ditixa Desai a *, Parth Soni a, Dinesh Shah b, Mark Willcox c, Furqan Maulvi a
a Maliba Pharmacy College, Uka Tarsadia University, Surat 394350, India
bDepartment of Chemical Engineering and Department of Anesthesiology, University of Florida, Gainesville, FL, USA 32611
cSchool of Optometry and Vision, University of New South Wales, Sydney, New South Wales 2052, Australia
* Corresponding author at: Maliba Pharmacy College, Uka Tarsadia University, Surat 394350, India
Abstract- Ocular drug delivery using contact lenses may be able to substitute for eye drop therapy. However, issues with hydrophobic drugs such as low drug uptake using a simple soaking method into preformed contact lenses and alteration in the swelling and transmittance of lenses restricts the application for drug delivery. This research uses graphene oxide (GO) to control the release of bimatoprost from contact lenses along with improvements in the drug uptake, and lens swelling and transmittance. GO was loaded into silicone hydrogel contact lenses during polymerization. These lenses when soaked in bimatoprost solution, improved its in vitro release profile. Adding both bimatoprost and GO during polymerization (DL-GO-BMT) significantly decreased the loss of drug during extraction and sterilization in comparison to contact lenses (DL-BMT) without GO. As the amount of GO was increased, the DL-GO-BMT lenses showed a significant decrease in the burst and cumulative release of bimatoprost. GO improved contact lens swelling due to its water binding capacity and lens transmittance due to the molecular dispersion of bimatoprost on the surface of the GO which prevented the local precipitation of the drug. Ocular irritation and histopathology reports demonstrated the safety of GO contact lens. The in vivo pharmacokinetic studies in the rabbit tear fluid showed significant improvement in MRT and AUC with DL-GO-0.2µg-BMT-100 contact lens in comparison to eye drop solution. The study demonstrated that the addition of GO to contact lenses can control the release of bimatoprost as well as improved the lens swelling and transmittance.
IMPLEMENTATION OF XGBOOST- A MACHINE LEARNING ALGORITHM TO OPTIMIZE THE SCREENED FORMULATIONS OF OPIOID ANALGESIC PRONIOSOMAL GEL
Sangeetha G1*, Swamivel Manickam M2, Sanil Kumar P3, Chandramouli R4
1Department of Pharmaceutics, Krupanidhi College of Pharmacy, Bengaluru-560035, Karnataka, India, 2Department of Pharmacy, Faculty of Engineering and Technology, Annamalai University, Tamil Nadu, India, 3Accenture, Bengaluru, Karnataka, India. 4Department of Quality Assurance, Krupanidhi College of Pharmacy, Bengaluru-560035, Karnataka, India
The abuse-forming potential of opioid analgesics is a matter of concern for formulators in this work. An opioid analgesic, tapentadol hydrochloride, is repurposed as a proniosomal gel using the principles of Parameter Sensitivity Analysis (PSA) assisted Main Effects Screening Design (MESD). The screened experiments were further computed with XG Boost, a machine learning algorithm for optimizing the best formulatory output given by PSA-assisted MESD. This work showcases the effectiveness of computational technologies and their potential applications for formulation design and optimization, which can be easily implemented and leveraged for faster and better formulation development.
SOLUBILITY ENHANCEMENT OF ITRACONAZOLE USING MESOPOROUS SILICA
Mugdha Pednekar, Dr. Swati Mittal , Saily Shinde*, Bhavisha Wadhwani
Department of Pharmaceutics, Vivekanand Education Society's College of Pharmacy, Hashu Advani Memorial Complex, Behind Collector Colony, Chembur, Mumbai, Maharashtra 400074
BCS class II drugs exhibit lower aqueous solubility, thereby limiting their oral bioavailability. Solubility is an integral part of any formulation in determining drug release and hence, drug absorption, which plays a key role in the oral bioavailability of formulations. The present study was attempted to enhance the solubility of one such poorly soluble drug- Itraconazole (ITZ) by loading it into the pores of mesoporous silica (Syloid® XDP 3050). The adsorbate of ITZ and mesoporous silica was further evaluated for drug loading, solubility enhancement and flow properties.
FORMULATION DEVELOPMENT OF SELF NANOEMULSIFYING OSMOTIC PUMP TABLETS (SNEOPT) OF FEUXOSTAT FOR CONTROLLED RELEASE
Bhagyashree Chande*, Rita Lala
Prin. K. M. Kundnani College of Pharmacy, Pharmaceutics Department, Mumbai: 400005, Maharashtra, India.
Self-Nano Emulsifying drug delivery system (SNEDDS) are considered to be a vibrant tool in solving low bioavailability issues of lipophilic drugs due to its poor solubility. Drugs used for the treatment of Gout exhibit solubility problems and hence incorporating them into nano carriers may show promising results in the treatment of Gout. Aim of current research work is to formulate, optimize, and develop stable SNEDDS for enhancing the solubility and bioavailability and also, Self-Nanoemulsifying Osmotic Pump Tablets (SNEOPT) for improving bioavailability and controlled drug release of Febuxostat which belongs to the class of xanthine oxidoreductase inhibitor (BCS Class II). L-SNEDDS was prepared by solubilizing drug in S mix and then in selected oil phase. Further adsorbing the L-SNEDDS onto solid carrier lead to formulation of S-SNEDDS. SNEOPT was prepared by Direct Compression method. Particle size of optimized batch was 97.25nm (LSNEDDS) and 155.2nm (S-SNEDDS). In vitro release from L-SNEDDS and S-SNEDDS was more than 75% in pH 1.2 and 80% in pH 7.4 in 1 hr. In vitro release from SNEOPT showed zero order drug release (more than 75% in 8 hrs). The optimized SNEDDS were found to be stable for 3 months at RT and refrigerated conditions.
ADVANCE TREATMENT APPROACH FOR ACUTE AND CHRONIC ALLERGIC FUNGAL RHINOSINUSITIS WITH THE HELP OF MODIFIED COMBINATION DRUG THERAPY
Vinayak Bhushan*, Suraj Singh S. Rathod*, Ritam Bandopadhyay*, Navneet Khurana, Awanish Mishra, Neha Sharma
School of Pharmaceutical Sciences, Lovely Professional University, Jalandhar - Delhi G.T. Road, Phagwara, Punjab (India)-144411
Allergic Fungal Rhinosinusitis (AFRS) could be a significantly perceived mark for a sort of polypoid Chronic rhinosinusitis (CRS) that's portrayed by type 1 hypersensitivity the buildup of dense inspissated “eosinophilic mucin” and trapped fungi within the sinuses. Endoscopic surgical clearance is required in most cases of AFRS. Medical treatment for AFRS is crucial to get future symptomatic control, retard polyp re-growth, and delay or prevent revision surgery. Systemic anti-inflammatory agents and anti-fungal agents are usually required within the treatment of AFRS and appear to be the foremost effective medical therapy. This study aimed to organize a nasal dosage form by fluticasone propionate and itraconazole for allergic fungal rhinosinusitis by an appropriate method. Their activity is additionally predicted using PASS software and with the assistance of their prediction, the fluticasone propionate and Itraconazole were prepared from various sets of ingredients including the suspending agents like microcrystalline cellulose, sodium carboxymethylcellulose, polyethylene glycol 400, etc. The formulations were evaluated first for the trial batch and then for the final batch also the formulation was further evaluated to optimize the drop size and concentration of chitosan for better absorption of the drugs.