Antifungal Topical Nanoemulgel Containing Miconazole Nitrate

Nanomulgel have emerged as one of the most interesting topical drug delivery system as it has dual release control system i.e. nanoemulsion and gel. Also the stability of nanoemulsion is increased when it is incorporated in gel. Miconazole nitrate is an antifungal medication topically administered to treat skin infections such as athlete’s foot, jock itch and ringworm. The aim of the present research work was to investigate the potential of nanoemulgel in enhancing the topical delivery of hydrophobic drug. MCZ nanoemulsions were prepared using span 80, tween 80, propylene glycol and different conc. of sunflower oil by High pressure homogenization technique. The prepared nanoemulsions were evaluated for pH, drug content, centrifugation, globule size and zeta potential.F2 showed highest drug content 91.26%.The globule size are found to be satisfactory range of nanoemulsion. The drug release kinetics is in the order of F2>F3>F4>F5>F1.And Nanoemulgel is prepared by using Carbopol 934 as gelling agent The release kinetics of nanoemulgel was found to obey zero order kinetics. The nanoemulgel was found to be stable with respect to physical appearance, pH, rheological properties spreadability and drug content at all temperature and conditions for two month. Hence, in the present study it can be concluded that Miconazole Nitrate nanoemulgel formulation is a promising system for the topical drug delivery and also an alternative method to deliver the hydrophobic drugs in water soluble gel bases. Key words: Hydrophobic drugs, Nanoemulgel, Miconazole nitrate, Topical drug delivery.

Liposomes as Vancomycin Hydrochloride Delivery System

Liposomes are being used as unique drug delivery systems due to their ability to encapsulate both hydrophilic and hydrophobic drugs, as well as for the fact that they improve the disadvantages of free drug administration. However, liposomes have a significant disadvantage - low encapsulation efficiency. In the research carried out, 1,2-distearoyl-sn-glycero-3-phosphocholine (DSPC) and cholesterol (Chol), in the ratio (n/n) of 2:1, 3:1 and 4:1 respectively, were used to prepare the liposomes. Blank liposomes (LIP) and vancomycin hydrochloride (VANKA) containing liposomes (VANKA-LIP) were prepared for each of the DSPC and Chol compositions. The aim of our study was to evaluate the effect of liposome composition on the VANKA encapsulation efficiency and release kinetics.

Hyaluronan-Cholesterol Nanogels for the Enhancement of the Ocular Delivery of Therapeutics

The anatomy and physiology of the eye strongly limit the bioavailability of locally administered drugs. The entrapment of therapeutics into nanocarriers represents an effective strategy for the topical treatment of several ocular disorders, as they may protect the embedded molecules, enabling drug residence on the ocular surface and/or its penetration into different ocular compartments. The present work shows the activity of hyaluronan-cholesterol nanogels (NHs) as ocular permeation enhancers. Thanks to their bioadhesive properties, NHs firmly interact with the superficial corneal epithelium, without penetrating the stroma, thus modifying the transcorneal penetration of loaded therapeutics. Ex vivo transcorneal permeation experiments show that the permeation of hydrophilic drugs (i.e., tobramycin and diclofenac sodium salt), loaded in NHs, is significantly enhanced when compared to the free drug solutions. On the other side, the permeation of hydrophobic drugs (i.e., dexamethasone and piroxicam) is strongly dependent on the water solubility of the entrapped molecules. The obtained results suggest that NHs formulations can improve the ocular bioavailability of the instilled drugs by increasing their preocular retention time (hydrophobic drugs) or facilitating their permeation (hydrophilic drugs), thus opening the route for the application of HA-based NHs in the treatment of both anterior and posterior eye segment diseases.

Poloxamer 407 Based Gel Formulations for Transungual Delivery of Hydrophobic Drugs: Selection and Optimization of Potential Additives

The current study aimed to develop poloxamer 407 (P407) gel for transungual delivery of antifungal hydrophobic drugs with sufficient gel strength and drug loading. Gel strength and drug loading of P407 gel was improved by use of functional additives. Hydration enhancement effect was used to select optimum nail penetration enhancer. Face-centered central composite design (FCCCD) was used to observe the effect of the selected penetration enhancer (thioglycolic acid (TGA)) and cosolvent (ethanol) on gelation behavior to develop formulation with enough loading of hydrophobic drug, i.e., terbinafine HCl (TBN), and its permeation across the nail plate without compromising on gel strength. It was observed that increasing concentration of P407 and TGA significantly reduced gelation temperature and enhanced the gel strength of P407 gel and can be used to improve P407 gel strength. Under the scanning electron microscope, the significant effect of TGA as an ungual penetration enhancer was observed on the morphology of the nail plate. Optimized P407 gel prepared with modified cold method showed a gelation temperature of 8.7 ± 0.16 °C, gel strength of 122 ± 7.5 s and drug loading of 1.2% w/w, which was four times more than the drug loading in the gels prepared with conventional cold method. Rheological behavior was pseudoplastic with 47.75 ± 3.48% of gel erosion after 12 washings and 67.21 ± 2.16% of drug release after 12 h. A cumulative amount of TBN permeated from P407 gel with and without PE after 24 h was 27.30 ± 4.18 and 16.69 ± 2.31 µg/cm2, respectively. Thioglycolic acid can be used as a nail penetration enhancer without the chemical modification or addition of extra additives while retaining the gel strength. Water miscible cosolvents with moderate evaporability such as ethanol, can be incorporated to P407 gel by minor modification in method of preparation to load the required dose of hydrophobic drugs. Developed P407 gel formulation with sufficient gel strength and drug loading will be a promising carrier for transungual delivery of hydrophobic antifungal agents.