TOPICAL ANTI-PSORIATIC NANOPARTICULATE DRUG DELIVERY SYSTEM
Original Article
KIRAN BHISE
1*
, SHADAB KHAN
1
, GHAZALA MULLA
2
1
Department of Pharmaceutics, M. C. E. Society’s Allana College of Pharmacy, Pune, India,
2
Received: 03 Dec 2019, Revised and Accepted: 29 Jan 2020
Department of Physiology, Z. V. M. Unani
Medical College and Hospital, Pune, India
Email: ksbhise@rediffmail.com
ABSTRACT
Objective: Development of effective drug delivery in the treatment of psoriasis is the major challenge for its successful management. To develop
and assess the potential of Nanostructured Lipid Carriers (NLCs) enriched with the powdered leaves extracts of Azadirachta indica (AE), Lawsonia
inermis (LE) and fruit extract of Mallotus philippensis (ME) in the management of psoriasis.
Methods: Drug loaded NLCs were prepared via hot homogenization technique by adopting 2
3
Results: The optimized batch of NLCs was found within the nanosized range with a relatively low polydispersity index and zeta potential of-20mV.
The %EE for an optimized batch of NLCs was found to be 98.97±0.83%, 96.99±0.56% and 99.25±0.55% and the %DL of 21.84±0.15%, 8.55±045%,
and 87.91±0.38% respectively for AE, LE and ME.
factorial design with factors X1 as the concentration
of lipids, X2 concentration of surfactants and X3 being the number of homogenization cycle. The responses Y1 and Y2 were particle size and zeta
potential. The optimized batch was obtained from Surface response plot and was evaluated for zeta potential, % entrapment efficiency, % drug
loading, Scanning Electron Microscopy(SEM), % in vitro diffusion of drugs from the NLCs, anti-lipid peroxidation and nitric oxide scavenging
activities, cytotoxicity on HaCat cell lines, Mouse Tail and Rat ultraviolet ray B photodermatitis models for Psoriasis.
The SEM images showed the spherical vesicular structures of drugs loaded NLCs. The in-vitro diffusion of drugs from the NLCs followed initial burst
release thereafter sustained release for 24 h. The AE, LE and ME loaded NLCs proved to possess anti-lipid peroxidation and nitric oxide scavenging
activities, cytotoxicity on HaCat cell lines, DNA fragmentation on HaCat cell lines which are biomarkers in the pathogenesis of psoriasis. The results
of Mouse Tail and Rat ultraviolet ray B photodermatitis models for Psoriasis supported the anti-psoriatic potential of AE, LE and ME loaded NLCs.
Conclusion: AE, LE and ME loaded NLCs can be used for prolonged topical delivery to the psoriatic skin for an effective treatment.
Keywords: Psoriasis, Drug Extracts, Nanostructured Lipid Carriers, Evaluation
© 2020 The Authors. Published by Innovare Academic Sciences Pvt Ltd. This is an open-access article under the CC BY license (http://creativecommons.org/licenses/by/4.0/)
DOI: http://dx.doi.org/10.22159/ijap.2020v12i2.36536. Journal homepage: https://innovareacademics.in/journals/index.php/ijap
INTRODUCTION
Psoriasis is a common skin disease characterized by hyper-
proliferation of epidermal cells of skin [1]. Although extensive work
has been reported, the development of effective drug delivery is the
major challenge for the successful management of this disease [2-
27]. The barrier effect of skin offers several challenges for the topical
bioavailability from conventional formulations. The literature
review indicates the potential role of Nanostructured Lipid Carriers
(NLCs) in the topical treatment of psoriasis [20-27]. Attempts to use
topical allopathic treatments like corticosteroids, calcipotriene,
retinoids, coal tar, anthralin, clobetasol propionate, methotrexate,
cyclosporines have failed due to their toxicities and inappropriate
formulation design of the conventional dosage forms [28-30]. The
literature survey reveals that Azadirachta indica, Lawsonia
inermis, and Mallotus philippensis exhibit anti-inflammatory
activities in addition to their multitude of medicinal properties
and have been used in combination in traditional medicine in the
treatment of Psoriasis [31-35]. Different nanoparticulate drug
delivery systems of Azadirachta indica have been reported in the
literature such as Nanoemulsion, Nanocapsules, Solid lipid
nanoparticles, and the Niosomes and Silver Nanoparticles of
Lawsonia inermis leaves extract but no work has been done on
nanoparticulate drug delivery system of Mallotus philippensis [36-
40]. Also, the literature survey revealed the absence of
Azadirachta indica, Lawsonia inermis, and Mallotus philippensis
extracts loaded NLCs for the treatment of psoriasis. Therefore, the
present research was undertaken to investigate and assess the
potential of Nanostructured Lipid Carriers (NLCs) enriched with
the powdered leaves extracts of Azadirachta indica (AE), Lawsonia
inermis (LE) and fruit extract of Mallotus philippensis (ME)
respectively. In this study the authors have investigated the long-
term safety and efficacy of a three-compound formulation AE, LE
and ME extract for the treatment of psoriasis.
MATERIALS AND METHODS
Materials
The Dried herbs of Azadirachta indica Leaves, Lawsonia inermis Leaves
and Mallotus philippensis powder were purchased from local vendors
and authenticated (Ref No.: Bot/10/2017) from the Department of
Botany, Savitribai Phule University of Pune, India. The solid lipids were
obtained as gift samples from Gattefosse, France. Rest all chemicals were
of AR grade and were purchased from Sigma Aldrich.
Preparation of Azadirachta indica extract (AE), Lawsonia
inermis extract (LE) and Mallotus philippensis extract (ME)
loaded NLCs
The extracts were prepared from the leaves of Azadirachta indica
and Lawsonia inermis using the Soxhlet apparatus and that of
Mallotus philippensis fruits by maceration process and Drug loaded
NLCs were produced by hot high-pressure homogenization method
[41]. The factorial batches of AE, LE and ME loaded NLCs were
prepared by applying 2
3
Factorial Design [42] with factors, X1
(Stearic acid: Seasame oil, Mustard oil concentration), X2 (Tween80:
Span 20 concentration) and X3 (number of homogenization cycle) as
three independent variables at two levels–1 and+1. The two
dependent responses were Y1 (Particle size) and Y2 (Zeta Potential).
Accordingly, a total of eight formulations were designed and the
compositions of different formulations have been depicted in table
1. The pre-emulsion was prepared by thoroughly dissolving the ME
in the lipid phase containing stearic acid, sesame oil, mustard oil and
span 20 at 65 °C, the oil phase was immediately dispersed into the
hot aqueous phase consisting of Tween 80, AE and LE at 65 °C under
constant stirring at 8000 rpm for 20 min using Ultra Turrax IKA T25,
(Remi Motors Ltd, RM-12C Mumbai). For 2 gm of lipid mixture, 200
mg of AE, LE and ME mixture was taken in the ratio of 2.5:1:10. The
pre-emulsion was further processed by high-pressure homogenizer
International Journal of Applied Pharmaceutics
ISSN- 0975-7058 Vol 12, Issue 2, 2020