and evaluation of chitosan gel containing metformin-loaded polymeric nanoparticles for topical treatment of melanoma.

Objective: The purpose of this study was to prepare and evaluate chitosan (CS) gel containing metformin hydrochloride (MET)-loaded polycaprolactone (PCL) nanoparticles (NPs) for topical treatment of melanoma.

Significance: Topical administration of MET-PCL NPs-CS gel improves penetration of drug, decreases side effects, and increases efficacy of treatment.

Methods: MET-PCL NPs were prepared by double emulsion method.

Development of Oral Tablet Formulation Containing Erlotinib: Randomly Methylated-β-cyclodextrin Inclusion Complex Using Direct Compression Method.

Objectives: Erlotinib (ERL) is a tyrosine kinase inhibitor that has been used in the treatment of metastatic non-small cell lung cancer (NSCLC). However, its low aqueous solubility limits its absorption and oral bioavailability. To overcome these pharmacokinetic drawbacks, complexation of ERL can be applied.

Erlotinib complexation with randomly methylated -cyclodextrin improves drug solubility, intestinal permeability, and therapeutic efficacy in non-small cell lung cancer.

The purpose of this study was to investigate the impact of anticancer drug erlotinib-randomly methylated--cyclodextrin complex (ERL-RAMEB CD) on drug solubility and dissolution rate. Phase solubility study showed erlotinib displayed maximum solubility in RAMEB CD solution and the stability constant (K) was calculated to be 370 ± 16 M. The optimal formulation was obtained with ERL-RAMEB CD in a 1:1 molar ratio using the co-lyophilization technique.

Nanocapsules for Drug Delivery: An Updated Review of the Last Decade.

Background: For the past few decades, there has been considerable research interest in drug delivery strategies using nanoparticulate systems as carriers for a wide range of active pharmaceutical ingredients.

Objective: It is known that nanoparticulate drug delivery systems comprise a wide variety of dosage forms including nanospheres, micelles, solid lipid nanoparticles, nanoliposomes, dendrimers, magnetic nanoparticles, and nanocapsules.

Methods: This review describes nanocapsule preparation techniques and their applications for the treatment of several diseases using patents and examples from the literature.

Amphiphilic cyclodextrin nanoparticles.

Cyclodextrins are cyclic oligosaccharides obtained by enzymatic digestion of starch. The α-, β- and γ- cyclodextrins contain respectively 6, 7 and 8 glucopyranose units, with primary and secondary hydroxyl groups located on the narrow and wider rims of a truncated cone shape structure. Such structure is that of a hydrophobic inner cavity with a hydrophilic outer surface allowing to interact with a wide range of molecules like ions, protein and oligonucleotides to form inclusion complexes.

Therapeutic efficacy of folate receptor-targeted amphiphilic cyclodextrin nanoparticles as a novel vehicle for paclitaxel delivery in breast cancer.

Purpose: The aim of this study is to test folate-conjugated cyclodextrin nanoparticles (FCD-1 and FCD-2) as a vehicle for reducing toxicity and increasing the antitumor efficacy of paclitaxel especially for metastatic breast cancer.

Methods: For the evaluation of PCX-loaded FCD nanoparticles, animal studies were realised in terms of survival rate, tumour size, weight change, metastazis and histopathological examination.

Results: FCD-1 displayed significant advantages such as efficient targeting of folate receptor positive breast cancer cells and having considerably lower toxicity compared to that of Cremophor.

Amphiphilic Cyclodextrin Derivatives for Targeted Drug Delivery to Tumors.

Villiers has extensively studied cyclodextrins, a family of macrocyclic oligosaccharides linked by α-1,4 glycosidic bonds, in different fields since their discovery in 1891. The unique structure enabling inclusion complexation for natural cyclodextrins and cyclodextrin derivatives make them attractive for novel drug delivery systems. Cyclodextrins can be modified with long aliphatic chains to render an amphiphilic property and these different amphiphilic cyclodextrins are able to form nanoparticles without surfactants.

Design and optimization of novel paclitaxel-loaded folate-conjugated amphiphilic cyclodextrin nanoparticles.

As nanomedicines are gaining momentum in the therapy of cancer, new biomaterials emerge as alternative platforms for the delivery of anticancer drugs with bioavailability problems. In this study, two novel amphiphilic cyclodextrins (FCD-1 and FCD-2) conjugated with folate group to enable active targeting to folate positive breast tumors were introduced. The objective of this study was to develop and characterize new folated-CD nanoparticles via 3(2) factorial design for optimal final parameters.

Antitumor Efficacy of Bacillus Calmette-Guerin Loaded Cationic Nanoparticles for Intravesical Immunotherapy of Bladder Tumor Induced Rat Model.

For bladder cancer, intravesical chemo/immunotherapy is widely used as adjuvant therapy after surgical transurethral resection. Bacillus Calmette-Guerin (BCG) is a live attenuated Mycobacterium of the same family as tuberculosis, that is capable of inducing a local inflammatory response upon instillation into the bladder. Intravesical therapy with BCG has proved to be more effective in the prophylaxis and treatment of superficial bladder tumors than most chemotherapeutic agents used for the same indication.

Cationic core-shell nanoparticles for intravesical chemotherapy in tumor-induced rat model: safety and efficacy.

Mitomycin C (MMC) has shown potent efficacy against a wide spectrum of cancers and is clinical first choice in superficial bladder tumors. However, intravesical chemotherapy with MMC has been ineffective due to periodical discharge of the bladder and instability of this drug in acidic pH, both resulting in high rate of tumor recurrence and insufficiency to prevent progression. Nanocarriers may be a promising alternative for prolonged, effective and safe intravesical drug delivery due to their favorable size, surface properties and optimum interaction with mucosal layer of the bladder wall.

Prolonged retention and in vivo evaluation of cationic nanoparticles loaded with Mitomycin C designed for intravesical chemotherapy of bladder tumours.

To overcome the recurrence problem in bladder tumours; nanoparticles with positive surface charge may improve interaction with biological membranes for intravesical administration. The aim of this study was to design, develop and evaluate (in vitro-in vivo) cationic nanoparticles based on chitosan, poly-L-lysine or polycaprolactone for the effective intravesical delivery of chemotherapeutic agent MMC in a rat model. Poly-L-lysine-coated polycaprolactone nanoparticles and chitosan-coated polycaprolactone nanoparticles were prepared by the double emulsion technique.