Comparative in-vitro and in-vivo evaluation of spherulites and cubosomes of Irinotecan for lung targeting.

Aims: The present investigation aimed at the comparative evaluation of the developed nanocarriers, viz. spherulites and cubosomes for lung targeting.

Materials And Methods: Both the spherulites and cubosomes were characterized for their entrapment efficiency, drug loading, size and zeta potential, in-vitro drug release profile, surface morphology, hemocompatibility, and in-vivo pharmacokinetic and lung biodistribution.

Spherical crystal agglomeration technique for improved flow properties and oral bioavailability of atazanavir sulphate.

The current research focused on formulation of spherical crystal agglomerates (SCA) of atazanavir sulphate for improving flow property and solubility. SCA were formulated by quasi-emulsification solvent diffusion. Methanol, water and dichloromethane were employed as a good solvent, bad solvent and bridging liquid respectively.

Intranasal spray of cubosomal tizanidine hydrochloride for brain targeting: and characterisation.

Tizanidine HCl (TH) is used as first-line therapy for the treatment of muscular spasm. The intranasal cubosomal delivery system of TH for site-specific delivery, i.e.

Carboplatin-loaded ultradeformable vesicles for the management of endometrial cancer: and evaluation.

Present research work aimed to explore intravaginal route for the drug delivery for treatment of endometrial cancer (EC). Carboplatin (CBP)-loaded ultradeformable vesicle (CBP-UDV) was prepared and characterized for quality attributes and evaluated for its efficacy in rabbits using ultrasound imaging after intravaginal administration. The results showed that the formulation capable of carrying and localizing drug in uterus for prolonged period assisted by first uterine pass effect.

Formulation Development of Fast Dissolving Microneedles Loaded with Cubosomes of Febuxostat: In Vitro and In Vivo Evaluation.

Febuxostat is a widely prescribed drug for the treatment of gout, which is a highly prevalent disease worldwide and is a major cause of disability in mankind. Febuxostat suffers from several limitations such as gastrointestinal disturbances and low oral bioavailability. Thus, to improve patient compliance and bioavailability, transdermal drug delivery systems of Febuxostat were developed for obtaining enhanced permeation.

Formulation considerations for improving intranasal delivery of CNS acting therapeutics.

One of the principal impediments for the treatment of neurological conditions is the lack of ability of most of the medicinal agents to evade the blood-brain barrier. Among all the novel approaches to bypass the blood-brain barrier, nose to brain transport is the most patient compliant, non-invasive and effective approach. It directly transports drugs to the CNS via the trigeminal and olfactory nerves present in the nasal cavity.

Liposomes encapsulating novel antimicrobial peptide Omiganan: Characterization and its pharmacodynamic evaluation in atopic dermatitis and psoriasis mice model.

Omiganan is a novel 12 amino acid synthetic cationic peptide from the cathelicidin family. Omiganan possesses antimicrobial action against a wide range of microbes, including gram-positive and gram-negative bacteria and fungi. Omiganan mainly acts by depolarizing the cytoplasmic membrane, resulting in cellular disruption and death.

Design and pharmacodynamic evaluation of DPK-060 loaded Nanostructured lipid carrier embedded gel for dermal delivery: A novel approach in the treatment of atopic dermatitis.

DPK-060 is a synthetic, 17 amino acid peptide, structurally derived from the human protein kininogen. DPK-060 mainly acts by membrane disruption mechanism, thus demonstrating strong broad-spectrum antimicrobial activity against both gram-positive and gram-negative microbes, including methicillin-resistant S. aureus (MRSA) in-vitro and in-vivo.

Polymer-drug conjugates: Design principles, emerging synthetic strategies and clinical overview.

Adagen, an enzyme replacement treatment for adenosine deaminase deficiency, was the first protein-polymer conjugate to be approved in early 1990 s. Post this regulatory approval, numerous polymeric drugs and polymeric nanoparticles have entered the market as advanced or next-generation polymer-based therapeutics, while many others have currently been tested clinically. The polymer conjugation to therapeutic moiety offers several advantages, like enhanced solubilization of drug, controlled release, reduced immunogenicity, and prolonged circulation.

Investigation on Potential of Chitosan Nanoparticles for Oral Bioavailability Enhancement of Risedronate Sodium.

Risedronate sodium (RS) is used in osteoporosis for bone reabsorption. It is a BCS class III drug having poor oral bioavailability (<0.63%) due to low permeability.

Formulation and evaluation of raloxifene hydrochloride dry emulsion tablet using solid carrier adsorption technique.

The present study focused on the development of a dry emulsion tablet of raloxifene hydrochloride (RXF) using a solid carrier adsorption technique to enhance oral bioavailability. An oil-in-water emulsion was formulated and converted into dry powder using HPMC K4M plus Aerosil 200, then compressed into tablets. The prepared emulsion was evaluated for globule size, drug content and zeta potential.

QbD-driven development of dissolving microneedle patch loaded with ultradeformable liposomes encapsulated Noopept: Exploring a patient friendly, once-daily option to manage dementia.

Noopept (NPT), a potent neuroprotective agent, suffers the problem of poor oral bioavailability (~10%) and thus demands exploration of ways of bioavailability improvement. Present work focuses on confronting this issue via development of NPT loaded ultradeformable liposomes (UDL) and its further incorporation in fast dissolving microneedle patch (MNP) for transdermal route. A combination of Phospholipon 90 G and Phospholipon 90H was used as bilayer forming lipids while sodium deoxycholate was used as edge activator to formulate NPT UDL by ethanol injection method.

Development of intravaginal rod insert bearing liposomal raloxifene hydrochloride and Leuprolide acetate as a potential carrier for uterine targeting.

Objectives: This project aimed at the formulation of dual drug entrapped liposomes held as freeze-dried intravaginal rod insert (IVR), to be administered by vaginal route for uterine targeting.

Methods: Liposomes were formulated by dehydration-rehydration method using 3 : 1 molar ratio of1,2-distearoyl-sn-glycero-3-phosphocholine : Cholesterol. Characterization was done for vesicle size, zeta potential, entrapment efficiency, surface morphology and % loading.

Vinpocetine loaded ultradeformable liposomes as fast dissolving microneedle patch: Tackling treatment challenges of dementia.

Vinpocetine (VPN) displays poor bioavailability (~7%) and short half-life (2-3 h) justifying the frequent dosing requirement of currently marketed oral tablets (thrice daily) and thus, posing a great challenge to patient compliance. Present work envisaged to achieve an infusion like delivery through transdermal route so as to tackle aforesaid challenges. With this aim, ultradeformable liposomes (UDL) incorporated fast dissolving microneedle patch (MNP) of VPN was developed and optimized for vesicle size and percent drug entrapment (critical quality attributes, CQA) utilizing the quality by design tool.

Development of Solid Self-Microemulsifying System of Tizanidine Hydrochloride for Oral Bioavailability Enhancement: In Vitro and In Vivo Evaluation.

The aim of the present investigation was to formulate self-microemulsifying drug delivery system (SMEDDS) tablets to enhance the oral bioavailability of tizanidine hydrochloride. SMEDDS was prepared by using Capmul G as the oil phase, Tween 20 as the surfactant, and propylene glycol as the co-surfactant. The optimized formulation was characterized by dilution test, % transmittance, thermodynamic stability, dye solubility, assay, globule size, zeta potential, and TEM.

Formulation and evaluation of liquisolid compacts of itraconazole to enhance its oral bioavailability.

Formulate and evaluate liquisolid compacts of Itraconazole, a biopharmaceutical classification system class II drug, which has poor bioavailability. PEG 600 was used as a nonvolatile solvent, Alfacel PH 200 as a carrier and Aerosil 200 as a coating material. The Itraconazole solution upon mixing with a carrier and coating material resulted in a dry powder, which was compressed into tablets.

Microneedle-Mediated Transdermal Delivery of Tizanidine Hydrochloride.

Tizanidine hydrochloride is a skeletal muscle relaxant used for the treatment of spasm, a sudden involuntary muscle contraction leading to pain. The presently available oral dosage form has limitations such as high first pass metabolism resulting in low oral bioavailability. The short half-life necessitates its frequent administration to maintain the required plasma concentration.

Enhanced oral bioavailability and brain uptake of Darunavir using lipid nanoemulsion formulation.

The present work aimed to formulate Darunavir loaded lipid nanoemulsion to increase its oral bioavailability and enhance brain uptake. Various batches of lipid nanoemulsion of Darunavir were prepared by high pressure homogenization using soya bean oil, egg lecithin and Tween 80. The optimized batch DNE-3 had globule size of 109.

Tc-vinorelbine tartrate loaded spherulites: Lung disposition study in Sprague-Dawley rats by gamma scintigraphy.

Vinorelbine Tartrate (VLB) is the first line chemotherapeutic agent for treatment of Non-Small Cell Lung Cancer, whose non-specific distribution causes unwanted side effects. The aim of the present investigation was to formulate VLB loaded spherulites intended for targeting the lung. Spherulites were composed of Soyabean Phosphatidylcholine (SPC), Cholesterol (Chol), Potassium oleate and Mannitol.

Formulation of Technetium-labeled leuprolide loaded liposomes and its biodistribution study in New Zealand white female rabbits for assessment of its uterine targeting efficiency.

Leuprolide acetate (LPA), a GnRH analogue, is drug of choice for treatment of uterine fibroids and endometriosis. The current marketed formulations of LPA show severe systemic side effects. This project aims to formulate LPA loaded liposomes to be administered by vaginal route for uterine targeting.

Darunavir-Loaded Lipid Nanoparticles for Targeting to HIV Reservoirs.

Darunavir has a low oral bioavailability (37%) due to its lipophilic nature, metabolism by cytochrome P450 enzymes and P-gp efflux. Lipid nanoparticles were prepared in order to overcome its low bioavailability and to increase the binding efficacy of delivery system to the lymphoid system. Darunavir-loaded lipid nanoparticles were prepared using high-pressure homogenization technique.

Intranasal delivery of tapentadol hydrochloride-loaded chitosan nanoparticles: formulation, characterisation and its in vivo evaluation.

The aim of the present investigation was to formulate tapentadol hydrochloride-loaded chitosan nanoparticles (CS-NPs) for nose to brain delivery. Chitosan nanoparticles were prepared using ionotropic gelation technique. Optimisation of the formulation and process parameters was done using Box-Behnken Design.

Biodistribution study of Tc-gemcitabine-loaded spherulites in Sprague-Dawley rats by gamma scintigraphy to investigate its lung targeting potential.

Gemcitabine hydrochloride (GCH) is drug of choice for treatment of non-small cell lung cancer. This project aims to formulate GCH-loaded spherulites for lung targeting using soyabean phosphatidylcholine, cholesterol (Chol) and 1,2-distearoyl-sn-glycero-3-phosphoethanolamine-N-[amino(polyethylene glycol)-2000]. Vesicles were characterised for size, entrapment efficiency, drug release and in vitro cytotoxicity.

Statistically optimized fast dissolving microneedle transdermal patch of meloxicam: A patient friendly approach to manage arthritis.

Introduction: The long term administration of Meloxicam for the management of arthritis, a chronic disorder, results in gastrointestinal disturbances leading to poor patient compliance. Considering the favorable molecular weight, therapeutic dose, biological half-life and log P value of meloxicam for transdermal delivery, its fast dissolving microneedle patch, with an ability to breach the stratum corneum and efficiently deliver the cargo to deeper skin layers, were developed.

Methods: Microneedle patch of low molecular weight polyvinyl alcohol and polyvinylpyrrolidone was prepared using Polydimethylsiloxane micromolds.

Effect of particle size on oral bioavailability of darunavir-loaded solid lipid nanoparticles.

The present investigation aimed to study the effect of particle size of solid lipid nanoparticles (SLNs) on oral bioavailability of darunavir. High pressure homogenisation technique was used to prepare SLNs. Three different sized SLNs loaded with darunavir were developed with mean particle sizes of around 100 nm, 200 nm and 500 nm, respectively.