Probing influence of methodological variation on active loading of acetazolamide into nanoliposomes: biophysical, in vitro, ex vivo, in vivo and rheological investigation.

In the present work comparative evaluation of acetate and pH gradient techniques for effective drug loading in liposomes has been investigated. The acetazolamide (ACZ) loaded liposomes prepared by two methods were analyzed by vesicle size analysis, zeta potential, percent encapsulation efficiency, in vitro drug release studies and intraocular pressure lowering activity. ICH guidelines were followed for determining stability of the prepared liposomes. The superiority of acetate gradient method for active loading of acetazolamide has been established. The prepared acetate gradient positive liposomes showed extended hypotensive effect when compared to other liposomal formulations. Thus ACZ loaded liposomes prepared by acetate gradient technique may serve as promising ocular delivery system in the treatment of glaucoma. The current work emphasizes the fact that the techniques used for active drug loading into liposomes strongly influence the pharmaceutical performance of the final formulation.

Chitosan-reduced gold nanoparticles: a novel carrier for the preparation of spray-dried liposomes for topical delivery.

Exposure of skin to various chemical and physical agents results in excessive stress to the outermost cell layer of the skin, causing different degenerative effects that can be minimized by using antioxidant formulations. The major challenge, in this regard, is to develop a formulation, which can prevent photodegradation of the actives, thus allowing a significant amount to be deposited at the site. In recent decades, liposomal formulations have been extensively employed to overcome the barrier properties of the skin and photodegradation of actives. In the present study, chitosan-reduced gold nanoparticles were investigated for its potential as a carrier to prepare liposomes by a spray-drying method. Liposomes so obtained were characterized for phospholipid recovery, diffuse reflectance infrared Fourier transform (DRIFT) spectroscopy, particle size, zeta potential, encapsulation efficiency, and deposition of drug and gold nanoparticles in the rat skin. Further, a liposomal gel formulation was prepared using Carbopol® 980 NF (Noveon Systems, Kochi, India) and evaluated for drug deposition in the skin. Antioxidant activity of vitamin C encapsulated in gold liposomes was determined on a human leukemia (HL-60) cell line. The use of gold nanoparticles as a carrier showed improved phospholipid recovery and thus overcomes the liposome scalability problem. DRIFT spectra confirmed the presence of phospholipid in the formulation. Liposomal gel showed improved drug deposition, as compared to control and marketed preparations. A more interesting contribution of the chitosan-reduced gold nanoparticles was an enhanced antioxidant activity seen in case of the vitamin C-loaded gold liposomal formulation. Liposomal formulation was found to be stable for 3 months at 30°C and 65% relative humidity.

Development of vitamin loaded topical liposomal formulation using factorial design approach: drug deposition and stability.

Long-term exposure of the skin to UV light causes degenerative effects, which can be minimized by using antioxidant formulations. The major challenge in this regard is that a significant amount of antioxidant should reach at the site for effective photoprotection. However, barrier properties of the skin limit their use. In the present study, Vitamin E acetate was encapsulated into liposome for improving its topical delivery. However preparation of liposomes is very difficult due to number of formulation variables involved therein. In the present work systematic statistical study for the formulation of liposomes for topical delivery of Vitamin E using the factorial design approach was undertaken. Amount of phospholipid (PL) and cholesterol (CH) were taken at three different levels and liposomes were prepared using ethanol injection method. Liposomes were characterized for encapsulation efficiency, vesicle size, zeta potential, and drug deposition in the rat skin. Gels containing liposomal dispersion (batch with higher skin deposition of VE) were prepared in Carbopol 980 NF and were characterized for gel strength, viscosity and drug deposition in the rat skin. Stability of liposome dispersion and gel formulation was studied at 30 degrees C/65% RH for 3 months. Results of regression analysis revealed that vesicle size and drug deposition in the rat skin were dependent on the lipid concentration and lipid:drug ratio. Drug deposition in rat skin had an inverse relationship with respect to PL and CH concentration. Prepared liposomal dispersion (50 mg PL:6 mg CH) showed seven-fold increase in drug deposition compared to control (plain drug dispersion). Gel formulation demonstrated six-fold and four-fold increase in drug deposition compared to control gel and marketed cream, respectively. Liposome dispersion and gel formulation were found to be stable for 3 months. Factorial design was found to be well suited to identify the key variables affecting drug deposition. Improved drug deposition from liposomal preparations demonstrates its potential for dermal delivery.

Silk sericin as a moisturizer: an in vivo study.

BACKGROUND: Excessive transepidermal water loss (TEWL) is the one of the causes of dry skin, and skin moisturizers have been used to overcome it. AIM: The purpose of this research was to study the moisturizing effect of sericin, a silk protein. Because silk sericin has resemblance with the natural moisturizing factor (NMF), it has been studied for its application in skin cosmetics. METHODS: Sericin gels were prepared using sericin solution and with pluronic and carbopol as stabilizers. The gels were applied on the skin of healthy human volunteers and its moisturizing efficiency was evaluated by measuring the skin hydroxyproline content, impedance, TEWL, and scanning electron microscopy (SEM) results. RESULTS: Decrease in skin impedance, increase in hydroxyproline level, and hydration of epidermal cells revealed the moisturizing effect of sericin, whereas decrease in the value of TEWL may be attributed to occlusive effect, which prevents water loss from the upper layer of the skin. Skin surface topography revealed the smoothness of the upper layer of the skin as a result of moisturization. CONCLUSION: Increase in the intrinsic moisturization of skin by sericin may be attributed to restoration of the amino acids and its occlusive effect. Thus, it would become a promising and important moisturizing ingredient in moisturizing formulations.