Monoolein-based nanoparticles containing indinavir: a taste-masked drug delivery system.

OBJECTIVE: This study developed a novel child-friendly drug delivery system for pediatric HIV treatment: a liquid, taste-masked, and solvent-free monoolein-based nanoparticles formulation containing indinavir (0.1%). SIGNIFICANCE: Adherence to antiretroviral therapy by pediatric patients is difficult because of the lack of dosage forms adequate for children. METHODS: Monoolein-based nanoparticles were developed. The particle size, zeta potential, pH, drug content, small angle X-ray scattering, stability, in vitro drug release profile, biocompatibility, toxicity, and taste-masking properties were evaluated. RESULTS: Monoolein-based formulations containing indinavir had nanosized particles with 155 ± 7 nm, unimodal particle size distribution, and polydispersity index of 0.16 ± 0.03. The zeta potential was negative (-31.3 ± 0.3 mV) and pH was neutral (7.78 ± 0.01). A 96% drug incorporation efficiency was achieved, and the indinavir concentration remained constant for 30 days. Polarized light microscopy revealed isotropic characteristics. Transmission electron microscopy images showed spherical shaped morphology. Small-angle X-ray scattering displayed a form factor broad peak. Indinavir had a sustained release from the nanoparticles. The system was nonirritant and was able to mask drug bitter taste. CONCLUSIONS: Monoolein-based nanoparticles represent a suitable therapeutic strategy for antiretroviral treatment with the potential to reduce the frequency of drug administration and promote pediatric adherence.

Omeprazole nanoparticles suspension: Development of a stable liquid formulation with a view to pediatric administration.

Omeprazole (OME) is often used to treat disorders associated with gastric hypersecretion in children but a liquid pediatric formulation of this medicine is not currently available. The aim of this study is to develop OME loaded nanoparticles with a view to the obtention of a liquid pharmaceutical dosage form. Eudragit® RS100 was selected as the skeleton material in the inner core and pH-sensitive Eudragit® L100-55 was used as the outer coating of the nanoparticles prepared by the nanoprecipitation method. Pharmacological activity was evaluated by induction of ethanol ulcers in mice. The OME nanoparticles exhibited mean diameters of 174 nm (±17), polydispersity index of 0.229 (±0.01), zeta potential values of -13 mV (±2.60) and encapsulation efficiency of 68.1%. The in vivo pharmacological assessment showed the ability of nanoparticles to protect mice stomach against ulcer formation. The prepared suspension of OME nanoparticles represents effective therapeutic strategy in a liquid pharmaceutical form with the possibility of pediatric administration.

Improved sensory properties of a nanostructured ritonavir suspension with a pediatric administration perspective.

The pediatric adherence to antiretroviral therapy is critical to therapeutic success. Ritonavir, a protease inhibitor drug, is commercially available as an oral solution containing a high amount of ethanol and propylene glycol, contraindicated in children younger than 4 years. Moreover, this medicine presents a bitter taste, which is limiting for the adherence to treatment. This study aims to develop ritonavir nanoparticles followed by polymeric coating for sensory characteristics improvement. The nanoparticles were coated with Eudragit® L 100-55 and characterized. A human sensory panel evaluated the proposed formulations regarding its bitter taste. The formulation showed nanotechnological features, with 130 and 134 nm for ritonavir nanoparticles and ritonavir coated nanoparticles, respectively. The pH, zeta potential, drug content and encapsulation efficiency results were suitable for oral administration. The coated nanoparticles were capable of decreasing the drug bitter taste as shown in the sensory analysis. The ritonavir incorporation in nanoparticles, followed by polymer coating can be a reasonable strategy to obtain alcohol free taste-masked medicines, which are promising for pediatric therapy.

Evaluation of lipoic acid topical application on rats skin wound healing.

PURPOSE: To evaluate the effects of lipoic acid (thioctic acid) topical application on wound healing on rats skin, and the consequences of lipoic acid nanoencapsulation on this process. METHODS: The model used was the healing activity on wounds induced by surgical incision on rats skin (n = 44). The parameters analyzed (11 days) were wound healing rate and histology (vascular proliferation, polymorphonuclear or mononuclear cells, and collagen synthesis or reepithelialization), after application of free lipoic acid or lipoic acid- loaded nanocapsules. The antioxidant activity of these formulations was evaluated by lipid peroxidation test. RESULTS: It was demonstrated for the first time that the topical application of lipoic acid improves wound healing. On the seventh day after surgery, the animals treated with lipoic acid showed increased healing rate (60.7 ± 8.4%) compared to the negative control group (43.0 ± 17.4%), as so improvement of histological parameters. The nanoencapsulation reverted the pro-oxidant activity presented in vitro by lipoic acid, whereas diminished wound repair. CONCLUSIONS: The topical application of lipoic acid produced an increase in the skin wound healing, which may be related to its pro-oxidant activity. On the other hand, the nanoencapsulation of the lipoic acid reversed the pro-oxidant activity, although presented minor healing activity.

Evaluation of lipoic acid topical application on rats skin wound healing

PURPOSE: To evaluate the effects of lipoic acid (thioctic acid) topical application on wound healing on rats skin, and the consequences of lipoic acid nanoencapsulation on this process. METHODS: The model used was the healing activity on wounds induced by surgical incision on rats skin (n = 44). The parameters analyzed (11 days) were wound healing rate and histology (vascular proliferation, polymorphonuclear or mononuclear cells, and collagen synthesis or reepithelialization), after application of free lipoic acid or lipoic acid- loaded nanocapsules. The antioxidant activity of these formulations was evaluated by lipid peroxidation test. RESULTS: It was demonstrated for the first time that the topical application of lipoic acid improves wound healing. On the seventh day after surgery, the animals treated with lipoic acid showed increased healing rate (60.7 ± 8.4%) compared to the negative control group (43.0 ± 17.4%), as so improvement of histological parameters. The nanoencapsulation reverted the pro-oxidant activity presented in vitro by lipoic acid, whereas diminished wound repair. CONCLUSIONS: The topical application of lipoic acid produced an increase in the skin wound healing, which may be related to its pro-oxidant activity. On the other hand, the nanoencapsulation of the lipoic acid reversed the pro-oxidant activity, although presented minor healing activity.

Avaliação da qualidade de comprimidos de propranolol e enalapril distribuídos no sistema público de saúde em uma cidade do sul do Brasil / Evaluation of the quality of propranolol and enalapril tablets supplied in the public health system in a southern Brazilian city

A aquisição de medicamentos no serviço público de saúde brasileiro através de licitação com critério de menor preço gera preocupação com a qualidade dos produtos distribuídos à população. O objetivo deste trabalho foi avaliar a qualidade dos comprimidos de Enalapril 10 mg e Propranolol 40 mg adquiridos através de processo licitatório e distribuídos na rede pública de saúde de um município catarinense durante o período de um ano. Foram analisados: o aspecto visual, o peso médio, a friabilidade, o teor de fármaco e o tempo de dissolução. De um total de sete lotes, cinco apresentaram desvio da qualidade. Encontraram-se irregularidades no aspecto visual, peso médio, friabilidade e teor de princípio ativo. A avaliação dos medicamentos além de assegurar que os medicamentos dispensados na rede pública possuem qualidade e que podem ser utilizados com segurança pelos pacientes é também uma ferramenta para a qualificação de fornecedores e um subsídio para o aprimoramento do processo licitatório. Sugere-se a implantação de um sistema de gestão da qualidade que inclua a qualificação de fornecedores, o aperfeiçoamento do processo de licitação, incluindo especificações claras sobre a qualidade dos medicamentos adquiridos, bem como o monitoramento da qualidade integrado a ações de farmacovigilância.

The acquisition of medication by the Brazilian public health service through bidding processes based on the lowest price criterion is a source of concern with respect to the quality of the products offered to the population. The scope of this work was to evaluate the quality of Enalapril 10 mg and Propranolol 40 mg tablets bought via the bidding process and supplied by the public health system in a city in the state of Santa Catarina, Brasil, over the course of a year. The visual aspect, weight variation, friability, drug content and dissolving time were analyzed. Out of seven lots, five presented quality deviation. Irregularities were found in the visual aspect, weight variation, friability and active ingredient. The evaluation of the quality of medication, besides ensuring the quality of the products supplied by the health system and safe usage by patients, is also a tool to evaluate medical supply companies and ensure the enhancement of the bidding process. The implementation of a management system that includes the evaluation of medical supply companies, improvement of the bidding process with clear specifications about the quality of the medicines bought are all recommended to ensure product safety.

[Evaluation of the quality of propranolol and enalapril tablets supplied in the public health system in a southern Brazilian city]. / Avaliação da qualidade de comprimidos de propranolol e enalapril distribuídos no sistema público de saúde em uma cidade do sul do Brasil.

The acquisition of medication by the Brazilian public health service through bidding processes based on the lowest price criterion is a source of concern with respect to the quality of the products offered to the population. The scope of this work was to evaluate the quality of Enalapril 10 mg and Propranolol 40 mg tablets bought via the bidding process and supplied by the public health system in a city in the state of Santa Catarina, Brasil, over the course of a year. The visual aspect, weight variation, friability, drug content and dissolving time were analyzed. Out of seven lots, five presented quality deviation. Irregularities were found in the visual aspect, weight variation, friability and active ingredient. The evaluation of the quality of medication, besides ensuring the quality of the products supplied by the health system and safe usage by patients, is also a tool to evaluate medical supply companies and ensure the enhancement of the bidding process. The implementation of a management system that includes the evaluation of medical supply companies, improvement of the bidding process with clear specifications about the quality of the medicines bought are all recommended to ensure product safety.