scholarly journals PRONIOSOMES: A VESICULAR DRUG DELIVERY SYSTEM

Author(s):  
SARITHA M. ◽  
SATYA PRAKASH PANDA ◽  
SRAVANI BUDDHA ◽  
P. V. KAMALA KUMARI ◽  
Y. SRINIVASA RAO

In the development of new dosage forms, drug delivery using nanotechnology is playing a vital role. Vesicular drug delivery systems have gained wide attention in the field of nanotechnology, such as niosomes, liposomes and proniosomes. Among the vesicular carriers, proniosomes are superior. Proniosomes are water-soluble carrier particles that are coated with surfactant so these are dry formulations. They are rehydrated to use on agitation in hot aqueous media within minutes to form niosomal dispersion immediately. Both hydrophilic and lipophilic drugscan be incorporated into these proteasomes. The physical stability problems of niosomes like aggregation, fusion and leaking are minimized in proniosomes, routes, such as oral, parenteral, dermal and transdermal, ocular, oral mucosal, vaginal, pulmonary, and intranasal. Proniosomes prolong the existence of the drug in the systemic circulation and finally reduces toxicity. This review focuses on different aspects of proniosomes such as preparation, characterization, in vitro drug release, entrapment efficiency, applications in the present scenario in the market and future trends.

Author(s):  
Leena Jacob ◽  
Abhilash Tv ◽  
Shajan Abraham

Objective: The study was carried out with an objective to achieve a potential sustained release oral drug delivery system of an antihypertensive drug, Perindopril which is a ACE inhibitor having half life of 2 hours. Perindopril is water soluble drug, so we can control or delay the release rate of drug by using release retarding polymers. This may also decrease the toxic side effects by preventing the high initial concentration in the blood.Method: Microcapsules were prepared by solvent evaporation technique using Eudragit L100 and Ethyl cellulose as a retarding agent to control the release rate and magnesium stearate as an inert dispersing carrier to decrease the interfacial tension between lipophilic and hydrophilic phase. Results: Prepared microcapsules were evaluated for the particle size, percentage yield, drug entrapment efficiency, flow property and in vitro drug release for 12 h. Results indicated that the percentage yield, mean particle size, drug entrapment efficiency and the micrometric properties of the microcapsules was influenced by various drug: polymer ratio. The release rate of microcapsules could be controlled as desired by adjusting the combination ratio of dispersing agents to retarding agents.Conclusion:Perindopril microcapsules can be successfully designed to develop sustained drug delivery, that reduces the dosing frequency and their by one can increase the patient compliance.


2021 ◽  
Vol 11 (2-S) ◽  
pp. 76-81
Author(s):  
Jddtadmin Journal

Thepurpose of the study was to develop and evaluatemucoadhesive microspheres of Budesonide for pulmonary drug delivery systemhaving prolonged residence time and sustained drug release. Microspheres were prepared by emulsificationsolvent evaporation technique using HPMC, carbopol as polymers in varying ratios. The microspheres were evaluated for its percentage yield, drug entrapment efficiency, particle size and shape, in vitro mucoadhesion study and in vitro drug release studies.The FTIR studies revealed no chemical interaction between the drug molecule and polymers and found that drug was compatible with used polymer. The mucoadhesive microspheres showed particle size, drug entrapment efficiency and yield in the ranges of148 - 164 μm, 68.0 - 85.0%and67.52 - 87.25% respectively. In vitro drug release and mucoadhesion study confirms thatformulationF5 was the best formulation as it releases 81.8 % at the end of 12 hr. in controlled manner and percentage mucoadhesion of 75.2 % after 10 hr. This confirms the developed budesonidemucoadhesive microspheres are promising for pulmonary drug delivery system.   Keywords: Budesonide, Mucoadhesion, Microspheres, Drug entrapment efficiency.


Author(s):  
Risvana Iqubal ◽  
Vimal Mathew ◽  
Kumar M. ◽  
Najiya Nasri K. V. ◽  
Safeetha Shamsudheen ◽  
...  

The poor penetration rate of the skin as a natural barrier makes transdermal drug delivery problematic. To increase transdermal dispersion of bioactives, electrophoresis, iontophoresis, chemical permeation enhancers, microneedles, sonophoresis, and vesicular systems such as liposomes, niosomes, elastic liposomes such as ethosomes, and transferosomes have all been used. Among these, transferosomes appear to be a promising option. Transferosomes are elastomeric or deformable vesicles that were originally discovered in the early 1990s. They're novel vesicular drug carrier system composed of phospholipid, surfactant, and water that improves transdermal drug delivery. Because of their low toxicity, biodegradability, ability to encapsulate both hydrophilic and lipophilic molecules, ability to prolong the drug's existence in the systemic circulation by encapsulation in vesicles, ability to target organs and tissues, and ability to reduce drug toxicity while increasing bioavailability, these vesicles are preferred over others. These vesicles undergo deformation, changes its shape and easily penetrates through the skin pores. There are two phases in any technique for preparing transferosomes. First, a thin film is hydrated before being sonicated to the required size; next, sonicated vesicles are homogenized by extrusion through a polycarbonate membrane. Transferosomes are evaluated for its entrapment efficiency, their drug content , in-vitro drug release, degree of deformability, turbidity, surface charge and morphology. Transferosomes are said to have a number of applications like delivery of vaccines,proteins, Anti-cancer drugs,anesthetics,herbal drugs and has better patient compliance,improved bio-availability and site-specific delivery and can serve as an emerging tool for transdermal delivery of almost all drugs and bio-actives.


Author(s):  
ANKITA TIWARI ◽  
SANJAY K. JAIN

Objective: The present investigation aimed to develop and characterize Eudragit S-100 coated alginate beads bearing oxaliplatin loaded liposomes for colon-specific drug delivery. Methods: Liposomes were formulated by the thin-film hydration method. The process and formulation variables were optimized by Box-Behnken design (BBD) with the help of Design-Expert® Software. Three independent variables taken were HSPC: Chol molar ratio (X1), hydration time (X2), and sonication time (X3). The response variables selected were entrapment efficiency of oxaliplatin, polydispersity index, and vesicle size. Results: The liposomes possessed an average vesicle size of 110.1±2.8 nm, PDI 0.096±0.3, zeta potential of-6.70±1.4 mV, and entrapment efficiency of 27.65%. The beads were characterized for their size, in vitro drug release, and swelling index. The degree of swelling of the beads was found to be 2.3 fold higher at pH 7.4 than at pH 1.2. The in vitro drug release depicted a sustained drug release in 48 h. Conclusion: The outcomes of the study proposed that the developed system can be effectively used for site-specific drug delivery to the colon via the oral route.


Author(s):  
Swapna Velivela ◽  
Nikunja B Pati ◽  
B. Ravindra Babu

Temozolomide is an anti-cancer drug; it was encapsulated in liposomal intravenous application. To avoid the side effects and to target the drug to the specific site, we have formulated liposomal formulation of Temozolomide. The liposomal were prepared by dried thin film hydration technique using rotary evaporator with drug and Soya phosphatidyl choline as carrier. The prepared liposomes were characterized for size, shape, % entrapment efficiency, in-vitro drug release and physical stability. The evaluated batches showed good physicochemical characteristics. The maximum encapsulation efficiency of Temozolomide was achieved with formulation TMZ 6 with 40.19% and the in-vitro drug release is 64.94%. Based on the results it can be concluded that TMZ 6 was selected as optimized formulation and the optimized formulation Optimized formulation follows zero order release kinetics and follow super case II transport when it applied to Korsmeyer-Pepps model for mechanism of drug release.


Author(s):  
J. Venkateswara Rao ◽  
T. Rama Mohan Reddy

In the present study, we sought to improve the solubility and bioavailability of lercanidipine HCl using self-nanoemulsifying drug delivery systems (SNEDDS). The extent of self-emulsification was checked with various oils with suitable surfactants and co-surfactants. The final optimized formulation contained Caproyl 90, Tween 80 and Labrosol as oil, surfactant and co-surfactant respectively. Based on lercanidipine solubility analysis, ternary phase diagrams were constructed for optimizing the system. The formulations were evaluated for FTIR studies, scanning electron microscopy (SEM), solubility, droplet size determination, zeta potential and stability studies. The droplet size was found to be 5.1 nm and Z-Average of 14.6 nm. The zeta potential of the optimized formulation (F16) was found to be -19.7 mV. In vitro drug release from SNEDDS was significantly higher than pure drug. Hence, lercanidipine SNEDDS is an optimum formulation strategy to enhance the solubility and oral bioavailability of this poorly water-soluble drug.


Author(s):  
Rakesh Patel ◽  
Hardik Patel ◽  
Ashok Baria

Antifungal drug, Ketoconazole was encapsulated in liposomes for topical application. Ketoconazole liposomes were prepared by thin film hydration technique using soya lecithin, cholesterol and drug in different weight ratios. The prepared liposomes were characterized for size, shape, entrapment efficiency, in-vitro drug release (by franz diffusion cell) and physical stability. The studies demonstrated successful preparation of Ketoconazole liposomes and effect of soya lecithin: cholesterol weight ratio on entrapment efficiency and on drug release.


Author(s):  
JAMPALA RAJKUMAR ◽  
G.V. RADHA ◽  
S. GANAPATY

Objective: This work aimed to establish and formulate the gossypinproniosomal gel drug delivery system. Methods: Gossypin-loaded proniosomal gels (GPG) was prepared using specific non-ionic surfactants (Spans), followed by particle size (PS), entrapment efficiency (percent EE), in vitro, ex-vivo drug release, and in vitro efficacy of Gossypin against human melanoma cells (A-375). Results: The results showed that the percentage EE for the GPG is appropriate (81.3 %–95.5 %) and they are Nano-sized (189.3–912.0 nm) and the gels diffusion provided the desired sustaining effect for GPG-F7 formulation (75.5 percent). The GPG reported cell viability of 14.9±2.3 percent compared with 16.1±1.1 percent for free Gossypin at the maximum dose of 100 μg/ml for A-375 human melanoma cells after 24 hr incubation time. No major changes were seen in the percentage EE, PS of GPG after storage for 90d, in the physical stability report. Conclusion: The results obtained suggest that the proniosomal drug delivery system can enhance the flux to the skin and achieve the ideal Gossypin sustainability effect. Consequently, the use of proniosomal gel may be advantageous with regard to the topical delivery of Gossypin for melanoma treatment management.


e-Polymers ◽  
2008 ◽  
Vol 8 (1) ◽  
Author(s):  
Mehrdad Mahkam

AbstractNew biodegradable polymeric hydrogels based on biocompatible materials, glucose acrylate (GA) and methacrylic acid (MAA) were designed and synthesized. In the first time, the glucose-6-acrylate-1,2,3,4-tetraacetate (GATA) monomer was prepared under mild conditions. The removal of protecting acetate groups from GATA will be carried out before the polymerization and then, the corresponding water soluble glycomonomer (GA) was obtained. This deprotected glycomonomer can be polymerized in aqueous media, which points to a way to obtain polymers with applications in biomedical and biochemical fields. Hydrogel synthesis was carried out by free-radical polymerization of the co-monomers using persulfate as an initiator and N,N′-methylenebisacrylamide as crosslinker. The hydrogels was characterized by FT-IR. Equilibrium swelling studies were carried out in enzyme-free simulated gastric and intestinal fluids (SGF and SIF, respectively). The swelling behaviour of the copolymers was dependent on the content of MAA groups and caused a decrease in gel swelling in pH 1 or an increase in gel swelling in pH 7.4. Model drug, 5-aminosalicylic acid (5-ASA) was entrapped into these hydrogels and the in vitro release profile of this drug was established separately in both enzyme-free SGF and SIF. Based on the great difference in swelling ratio at pH 1 and 7.4 for these hydrogels, it appears to be good candidates for colon-specific drug delivery.


2021 ◽  
Author(s):  
Archana Patil ◽  
Vedangi Tuencar ◽  
Anand Gadad ◽  
Panchaxari Dandagi ◽  
Rajashree Masareddy

Background: Nanostructured lipid carriers (NLCs) of fluconazole were prepared to improve permeability and thereby effective topical drug delivery. Materials and method: NLCs were prepared and evaluated, and then the optimized NLC suspension was incorporated into a gel that was further evaluated for topical drug delivery. Results and discussion: F-2 NLC formulation was optimized based on results of particle size (161.3 ± 1.385 nm), polydispersity index (0.401), zeta potential (-33 ± 0.46), entrapment efficiency (82.26 ± 0.91%) and in vitro drug release (76.40 ± 0.21%). Ex vivo skin permeation studies showed flux of F-2 gel and the comparison marketed gel as 0.21 and 0.18 mg/cm2/h, respectively. The in vitro antifungal study revealed significantly better activity compared with the marketed gel. Conclusion: Fluconazole NLCs increase drug permeability and proved to be effective in topical drug delivery.


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