Current trends in pharmaceutical treatment of dry eye disease: A review.

Dry eye disease (DED), keratoconjunctivitis sicca or dysfunctional tear syndrome, is the most prevalent ophthalmic disease which affects a substantial segment of people worldwide with increasing frequency. It is considered a multifactorial disease of the ocular surface and tear film, characterized by a variation of signs and symptoms. The symptoms range from mild to severe itching, burning, irritation, eye fatigue, and ocular inflammation that may lead to potential damage to the cornea, conjunctiva and even vision loss. Correspondingly, depending on the different manifestations and pathophysiology, the treatment must be tailored specifically to each patient by targeting the specific mechanisms implicated in their disease. Currently, there are several medical products and techniques available or under investigation for the treatment of DED. The present article focused on the pathophysiology of DED, the new diagnostic approach and the recently developed drug delivery systems or devices reducing the progress of the disease and treating the causes.

Vaginal suppositories of cumin seeds essential oil for treatment of vaginal candidiasis: Formulation, in vitro, in vivo, and clinical evaluation.

Fungal infections by resistant Candida species continue to be a significant health problem. Novel antifungal agents such as essential oils of cumin seeds (EOCS) are tested against vulvovaginal candidiasis (VVC). The aim of this study was to develop coated polyethylene glycol (PEG) vaginal suppositories containing EOCS for treatment of VVC. PEG suppositories containing EOCS were prepared ppearance, weight variation, drug content, hardness, dissolution time, release, stability and anticandida activity were evaluated. Biocompatibility of selected formulation was tested in female rabbits, followed by clinical evaluation. Coated suppositories showed complete release of the oil after 30 min, in vitro anti-candida activity, enhanced stability and sufficient safety on the vaginal tissues of rabbits. Clinical results showed significant lower rates of vaginal itching, discharge and dyspareunia combined with negative cultures in 70% of patients, revealing efficacy of EOCS-containing vaginal suppositories for treatment of VVC.

Spidroin in carbopol-based gel promotes wound healing in earthworm's skin model.

Spider silk's regenerative, biocompatible, and antimicrobial properties render it a promising biomaterial for wound healing promotion. Spidroin as the main protein component of spider silks was used in this study to evaluate the potential effects on wound healing via topical application of novel spidroin-containing carbopol 934 (CP934) gel. Spidroin was extracted, formulated into CP934 gel, and characterized both in vitro and in vivo. Spidroin gel was translucent and brownish-yellow in color. An optimum viscosity was obtained at 0.6% CP934 at neutral pH. Optimized spidroin gel (0.6% CP934) effectively inhibited the growth of clinical bacterial isolates of methicillin-sensitive Staphylococcus aureus (MSSA), methicillin-resistant S. aureus (MRSA) and Escherichia coli at 440 µg/mL with MIC values of 0.98, 4.6, and 8.2 µg/mL, respectively. Optimized spidroin gel was evaluated for wound healing via topical application on wounds surgically induced in Allolobophora caliginosa earthworms used as a robust human skin model. After application for three consecutive days, dramatic reductions in wound closure and reepithelialization duration were observed macroscopically and via histological studies (light and electron microscopy) when compared with control. In conclusion, these results show that spidroin gel is a promising promoter for wound healing, and further studies would be directed toward investigating mechanisms underlying this effect.

High payload nanostructured lipid carriers fabricated with alendronate/polyethyleneimine ion complexes.

Oral bioavailability of the anti-osteoporotic drug alendronate (AL) is limited to ≤ 1% due to unfavorable physicochemical properties. To augment absorption across the gastrointestinal mucosa, an ion pair complex between AL and polyethyleneimine (PEI) was formed and incorporated into nanostructured lipid carriers (NLCs) using a modified solvent injection method. When compared to free AL, ion pairing with PEI increased drug encapsulation efficiency in NLCs from 10% to 87%. Drug release from NLCs measured in vitro using fasted state simulated intestinal fluid, pH 6.5 (FaSSIF-V2) was significantly delayed after PEI complexation. Stability of AL/PEI was pH-dependent resulting in 10-fold faster dissociation of AL in FaSSIF-V2 than measured at pH 7.4. Intestinal permeation properties estimated in vitro across Caco-2 cell monolayers revealed a 3-fold greater flux of AL encapsulated as hydrophobic ion complex in NLCs when compared to AL solution (Papp = 8.43 ± 0.14 × 10-6 cm/s and vs. 2.76 ± 0.42 × 10-6 cm/s). Cellular safety of AL/PEI-containing NLCs was demonstrated up to an equivalent AL concentration of 2.5 mM. These results suggest that encapsulation of AL/PEI in NLCs appears a viable drug delivery strategy for augmenting oral bioavailability of this clinically relevant bisphosphonate drug and, simultaneously, increase gastrointestinal safety.